カルシウムチャネル

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1573	Fasudil (HA-1077) HCl	65 mg/mL	5 mg/mL	<1 mg/mL
S1356	Levetiracetam	34 mg/mL	34 mg/mL	34 mg/mL
S1813	Amlodipine Besylate	<1 mg/mL	113 mg/mL	14 mg/mL
S1293	Cilnidipine	<1 mg/mL	99 mg/mL	15 mg/mL
S1811	Amiloride HCl	6 mg/mL	53 mg/mL	5 mg/mL
S6920	SEA0400	<1 mg/mL	74 mg/mL	74 mg/mL
S3242	Loureirin B	-1 mg/mL	100 mg/mL	-1 mg/mL
S6847	ML-9 HCl	10 mg/mL	72 mg/mL	6 mg/mL
S6834	CM 4620	-1 mg/mL	100 mg/mL	-1 mg/mL
S0016	SN-6	<1 mg/mL	80 mg/mL	<1 mg/mL
S0000	Cav 2.2 blocker 1	<1 mg/mL	12 mg/mL	15 mg/mL
S1425	Ranolazine 2HCl	100 mg/mL	100 mg/mL	<1 mg/mL
S4202	Verapamil HCl	50 mg/mL	98 mg/mL	12 mg/mL
S2482	Manidipine 2HCl	<1 mg/mL	21 mg/mL	<1 mg/mL
S1799	Ranolazine	<1 mg/mL	86 mg/mL	20 mg/mL
S1662	Isradipine	<1 mg/mL	74 mg/mL	74 mg/mL
S1905	Amlodipine	<1 mg/mL	82 mg/mL	82 mg/mL
S1885	Felodipine	<1 mg/mL	77 mg/mL	72 mg/mL
S2481	Manidipine	<1 mg/mL	122 mg/mL	3 mg/mL
S1748	Nisoldipine	<1 mg/mL	77 mg/mL	60 mg/mL
S1747	Nimodipine	<1 mg/mL	84 mg/mL	84 mg/mL
S2721	Nilvadipine	<1 mg/mL	77 mg/mL	33 mg/mL
S1994	Lacidipine	<1 mg/mL	91 mg/mL	22 mg/mL
S2114	Dronedarone HCl	<1 mg/mL	80 mg/mL	40 mg/mL
S4181	Nicardipine HCl	<1 mg/mL	100 mg/mL	<1 mg/mL
S1808	Nifedipine	<1 mg/mL	69 mg/mL	15 mg/mL
S2080	Clevidipine Butyrate	<1 mg/mL	91 mg/mL	3 mg/mL
S2017	Benidipine HCl	<1 mg/mL	8 mg/mL	<1 mg/mL
S2030	Flunarizine 2HCl	<1 mg/mL	5 mg/mL	'3 mg/mL
S2491	Nitrendipine	<1 mg/mL	72 mg/mL	<1 mg/mL
S3053	Azelnidipine	<1 mg/mL	117 mg/mL	7 mg/mL
S2573	Tetracaine HCl	60 mg/mL	60 mg/mL	30 mg/mL
S1865	Diltiazem HCl	90 mg/mL	90 mg/mL	4 mg/mL
S3045	Cinepazide maleate	107 mg/mL	107 mg/mL	<1 mg/mL
S5255	Nicardipine	30 mg/mL	95 mg/mL	95 mg/mL
S8380	YM-58483 (BTP2)	<1 mg/mL	84 mg/mL	84 mg/mL
S6657	2-Aminoethyl Diphenylborinate (2-APB)	<1 mg/mL	45 mg/mL	23 mg/mL
S4626	Ethosuximide	28 mg/mL	28 mg/mL	28 mg/mL
S4597	Lercanidipine hydrochloride	<1 mg/mL	66 mg/mL	1 mg/mL
S4977	Efonidipine	-1 mg/mL	100 mg/mL	40 mg/mL
S5279	Fendiline hydrochloride	-1 mg/mL	70 mg/mL	-1 mg/mL
S3845	Panaxadiol	<1 mg/mL	<1 mg/mL	22 mg/mL
S3700	DHBP dibromide	100 mg/mL	100 mg/mL	'100 mg/mL
S2403	Tetrandrine	<1 mg/mL	1 mg/mL	2 mg/mL
S9315	Praeruptorin A	-1 mg/mL	77 mg/mL	-1 mg/mL
S3931	Ginsenoside Rd	-1 mg/mL	90 mg/mL	-1 mg/mL
S5514	Lanthanum(III) chloride heptahydrate	-1 mg/mL	50 mg/mL	-1 mg/mL
S3766	Tanshinone IIA sulfonate sodium	-1 mg/mL	79 mg/mL	-1 mg/mL
S4084	Lomerizine 2HCl	<1 mg/mL	100 mg/mL	52 mg/mL
S4648	Dantrolene sodium hemiheptahydrate	<1 mg/mL	14 mg/mL	<1 mg/mL
S3682	Ethyl 3-Aminobenzoate methanesulfonate	52 mg/mL	52 mg/mL	52 mg/mL
S9400	Rhynchophylline	-1 mg/mL	76 mg/mL	-1 mg/mL
S3674	Levamlodipine	81 mg/mL	81 mg/mL	81 mg/mL
S3883	Protopine	-1 mg/mL	30 mg/mL	-1 mg/mL
S5567	Trimethadione	-1 mg/mL	28 mg/mL	-1 mg/mL
S9566	Bepridil hydrochloride	-1 mg/mL	41 mg/mL	-1 mg/mL
S6473	Pinaverium bromide	16 mg/mL	100 mg/mL	'100 mg/mL
S4727	Cinnarizine	<1 mg/mL	73 mg/mL	'<1 mg/mL
S2050	Strontium Ranelate	<1 mg/mL	<1 mg/mL	<1 mg/mL
S7924	Bay K 8644	<1 mg/mL	71 mg/mL	71 mg/mL
S4209	Chlorocresol	<1 mg/mL	29 mg/mL	29 mg/mL
S0870	Barnidipine	<1 mg/mL	98 mg/mL	'''<1 mg/mL
S2436	Pranidipine	<1 mg/mL	90 mg/mL	2 mg/mL
S4931	Propiverine hydrochloride	-1 mg/mL	80 mg/mL	-1 mg/mL
S3809	Imperatorin	-1 mg/mL	54 mg/mL	-1 mg/mL
S2953	Dooku1	<1 mg/mL	65 mg/mL	5 mg/mL
S5861	Lercanidipine	<1 mg/mL	55 mg/mL	<1 mg/mL
S9151	Praeruptorin E	-1 mg/mL	34.6 mg/mL	-1 mg/mL
S3236	Mesaconitine	-1 mg/mL	12 mg/mL	-1 mg/mL
S0973	Wilforgine	-1 mg/mL	100 mg/mL	-1 mg/mL
S2535	Econazole nitrate	<1 mg/mL	89 mg/mL	5 mg/mL
S2415	Astragaloside A	<1 mg/mL	100 mg/mL	<1 mg/mL
S4353	Terfenadine	<1 mg/mL	94 mg/mL	27 mg/mL
S2446	Levosimendan	<1 mg/mL	56 mg/mL	<1 mg/mL
S1911	Disodium Cromoglycate	2 mg/mL	<1 mg/mL	<1 mg/mL
S5478	Dantrolene sodium	-1 mg/mL	67 mg/mL	-1 mg/mL

Calcium Channel製品

All (76) Calcium Channel阻害剤(58) Calcium Channel活性剤(3) Calcium Channel拮抗剤(6) Calcium Channel作動薬(1) Calcium Channelモジュレータ(5)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.	Nat Cell Biol, 2020, 25 Nat Commun, 2020, 11(1):71 Cell Rep, 2020, 30(11):3864-3874	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1356	Levetiracetam Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.	PLoS One, 2019, 14(2):e0211644 Sci Rep, 2016, 6:25705 Sci Rep, 2016, 6:25705	Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
S1813	Amlodipine Besylate Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.	Cell Discov, 2020, 6(1):96 Oncogene, 2019, 38(1):120-139
S1293	Cilnidipine Cilnidipine (FRC-8653) is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96 Res Sq, 2020, rs.3.rs-48659
S1811	Amiloride HCl Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).	Signal Transduct Target Ther, 2020, 5(1):214 PLoS Genet, 2020, 16(10):e1009100 Drug Discov Ther, 2020, 14(5):256-258
S6920^新	SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S3242^新	Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the K_ATP current, influx of Ca²⁺ to the intracellular.
S6847^新	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.	J Mol Endocrinol, 2019, 63(3):199-213
S6834^新	CM 4620 CM 4620 is an inhibitor of calcium-release activated calcium-channel (CRAC channel). CM4620 inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of near 120 nM and 900 nM, respectively.
S0016^新	SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S0000^新	Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 0.001 μM.
S1425	Ranolazine 2HCl Ranolazine 2HCl (RS-43285) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.	Front Pharmacol, 2019, 10:1367
S4202	Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.	Nat Commun, 2019, 10(1):3838 Clin Cancer Res, 2019, clincanres.1768.2019 EBioMedicine, 2019, 48:70-80	The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
S2482	Manidipine 2HCl Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.		Manidipine decreases the accumulation of HCMV Early and Late proteins. HFFs were infected with HCMV AD169 and then treated with test compounds or DMSO as a control. NTZ-treated samples were also included as a control for inhibition of E and L protein expression. At the indicated times p.i., total cell extracts were prepared and analyzed by WB with anti-IEA, anti-UL44, and anti-UL99 antibodies. Tubulin immunodetection served as a loading control. Images are representative of three independent experiments.
S1799	Ranolazine Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
S1662	Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.	Cell Discov, 2020, 6(1):96 Drug Metab Dispos, 2015, 43(12):1934-7
S1905	Amlodipine Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.	ACS Infect Dis, 2020, acsinfecdis.0c00486 J Med Toxicol, 2020, 16(1):61-66 Oncogene, 2019, 38(1):120-139
S1885	Felodipine Felodipine (CGH-869) is a selective L-type Ca²⁺ channel blocker with IC50 of 0.15 nM.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96
S2481	Manidipine Manidipine is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive.	Antiviral Res, 2018, 150:130-136
S1748	Nisoldipine Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Ca_v1.2 with IC50 of 10 nM.	Cell Discov, 2020, 6(1):96 bioRxiv, 2020, 2020/9/20.4.7.30734
S1747	Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.	Cell Discov, 2020, 6(1):96 G3 (Bethesda), 2020, 4;10(5):1585-1597 Antiviral Res, 2016, 132:38-45	Assessment of the role of Ca2+ channels during RSV replication. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with calcium channel blockers nifedipine, nimodipine, and tetrandrine (A), at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. NS, no differences at a significance level of 0.05.
S2721	Nilvadipine Nilvadipine (ARC029, FR34235) is a potent calcium channel blocker with an IC50 of 0.03 nM.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1994	Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
S2114	Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).	Cell Syst, 2019, 8(2):97-108 Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
S4181	Nicardipine HCl Nicardipine HCl (RS-69216) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96
S1808	Nifedipine Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.	Cell Discov, 2020, 6(1):96 Front Pharmacol, 2019, 10:381 Biochem Biophys Res Commun, 2019, 509(1):76-81	The fold change of C-peptide content after octreotide, nicorandil and nifedipine treatment. Octreotide, nicorandil and nifedipine decreased insulin secretion in wild-type, heterozygous mutated and homozygous mutated cells.
S2080	Clevidipine Butyrate Clevidipine Butyrate is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure.	ACS Infect Dis, 2020, acsinfecdis.0c00486
S2017	Benidipine HCl Benidipine HCl (KW-3049) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96 Life Sci, 2019, 227:74-81
S2030	Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) is a dihydrochloride salt form which is a calcium channel blocker with a K_i of 68 nM.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S2491	Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
S3053	Azelnidipine Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker.
S2573	Tetracaine HCl Tetracaine HCl (Amethocalne) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor.
S1865	Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl is a benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions.	J Cell Mol Med, 2018, 22(12):5964-5977 FASEB J, 2017, 31(2):625-635	Gentisic acid reduces interstitial and perivascular fibrosis in mice with transverse aortic constriction (TAC). Representative images of Masson's trichrome staining of the hearts of mice in the sham and TAC + vehicle, gentisic acid, bisoprolol, or diltiazem groups. Scale bar = 50 μm. A, Interstitial fibrosis and B, perivascular fibrosis are shown. Fibrotic areas are stained blue.
S3045	Cinepazide maleate Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator.
S5255	Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
S8380	YM-58483 (BTP2) YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.	Cell Stem Cell, 2018, 22(6):865-878
S6657	2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.	Cell Discov, 2020, 6(1):96
S4626	Ethosuximide Ethosuximide is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker.	Nature, 2018, 554(7692):317-322	Antidepressant effects caused by systemic ethosuximide injection (200 mg kg−1, i.p.; c, d) in the FST(forced swim test) and SPT (sucrose preference test) 1 h after treatment.
S4597	Lercanidipine hydrochloride Lercanidipine is a calcium channel blocker of the dihydropyridine class.	J Phys Chem B, 2013, 117(23):6868-73
S4977	Efonidipine Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
S5279	Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845	Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S3700	DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium), a viologen for electrochromic memory display agent, inhibits the calcium release induced by 2 mM caffeine and 2 μg/ml polylysine with an IC50 value of 5 μg/ml and 4 μg/ml respectively.
S2403	Tetrandrine Tetrandrine (Fanchinine), a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a calcium channel blocker.	Nat Commun, 2020, 27;11(1):1620 Ann Transl Med, 2020, 8(16):1018 Cell Death Dis, 2019, 10(2):38	BMMs were seeded in a collage I-coated plate and incubated with RANKL (100 ng/ml) and M-CSF (50 ng/ml) for 5 d. When mature osteoclasts were observed, they were digested by collagenase and seeded on bovine bone slices. The bone slices were treated with or without tetrandrine for an additional 2 d. Then, the cells were stained with rhodamine–phalloidin to observe the F-actin rings, and the areas of F-actin rings were calculated by Image-Pro Plus 6.0 software.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S3931	Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
S5514	Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
S3766	Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
S4084	Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
S4648	Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) ia a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber.
S3682	Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) can block the generation of action potentials via voltage-dependent Na+-channels and usually used for anesthesia, sedation, or euthanasia of fish.
S9400	Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
S3674	Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
S3883	Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S5567	Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S9566	Bepridil hydrochloride Bepridil hydrochloride is an anti-anginal drug classified as a calcium channel blocker. It also blocks multiple other ion channels, including sodium and potassium channels.
S6473	Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.
S4727	Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.
S2050	Strontium Ranelate Strontium Ranelate is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.
S7924	Bay K 8644 Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.	J Cell Physiol, 2018, 10.1002/jcp.27791	Western blot analysis of myocardium lysate at 4 weeks. Hypertrophic markers were tested in mouse cardiomyocyte cell line HL-1 Bay-K-8644.
S4209	Chlorocresol Chlorocresol is an activator of ryanodine receptor.
S0870^新	Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) is an antihypertensive drug that belongs to the dihydropyridine (DHP) group of calcium antagonist (CaA) with Ki of 0.21 nM for [³H]nitrendipine binding sites.
S2436^新	Pranidipine Pranidipine is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta.
S4931	Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
S3809	Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.	Adv Sci (Weinh), 2020, 7(16):2000925 Theriogenology, 2019, 10.1016/j.theriogenology
S2953	Dooku1 Dooku1 is an analog of Yoda1 with antagonist activity against mechanosensitive Piezo1 channel. Dooku1 inhibits 2 μM Yoda1-induced Ca²⁺-entry with IC50 of 1.3 μM in HEK 293 cells and 1.5 μM in HUVECs, respectively.
S5861	Lercanidipine Lercanidipine is a vasoselective dihydropyridine calcium antagonist used for the treatment of essential hypertension.
S9151	Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.
S3236^新	Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S0973^新	Wilforgine Wilforgine, one of the major bioactive sesquiterpene alkaloids in Tripterygium wilfordii Hook. F., induces microstructural and ultrastructural changes in the muscles of M. separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
S2535	Econazole nitrate Econazole Nitrate (NSC 243115) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.	Biomol Ther (Seoul), 2020, 25
S2415	Astragaloside A Astragaloside A (Astragaloside IV) is the primary pure saponin isolated from Astragalus membranaceus, which has been widely used for the treatment of cardiovascular diseases.	Carcinogenesis, 2020, 41(7):993-1004 J Med Virol, 2019, 91(8):1440-1447
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S2446	Levosimendan Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.	Antiviral Res, 2017, 146:76-85	(B-E) The % of GFP-positive cells upon compound treatment were determined for the indicated HIV-1 latency cell lines (B. J-LAT 6.3; C. JLAT 10.6; D. CA5; E. EF7). Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6). * p < 0.05, one-way ANOVA followed by Tukey’s multiplecomparison test
S1911	Disodium Cromoglycate Disodium Cromoglycate (FPL 670, Cromolyn) is an antiallergic drug with IC50 of 39 μg/mL.
S5478	Dantrolene sodium Dantrolene sodium acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.	Sci Rep, 2019, 9(1):3487

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S1573	Fasudil (HA-1077) HCl Fasudil(HA-1077), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.	Nat Cell Biol, 2020, 25 Nat Commun, 2020, 11(1):71 Cell Rep, 2020, 30(11):3864-3874	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1356	Levetiracetam Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy. Levetiracetam (UCB-L059, SIB-S1) is an agonist of muscarinic acetylcholine receptors (mAChR). Levetiracetam modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.	PLoS One, 2019, 14(2):e0211644 Sci Rep, 2016, 6:25705 Sci Rep, 2016, 6:25705	Levetiracetam reduces DNA, synaptic, and neurite damage caused by Dox. (A) An example of cortical cultures pre-treated with 5 μ M Lev and then Dox (0.01 μ M, overnight), fixed and stained with antibodies against MAP2c. Scale bar is 20 μ m. (B) Cortical neurons at 28–32 DIV were pre-treated with 5 μ M Lev, and then a vehicle or with Dox (0.01 μ M for 3 days, or 0.1 μ M, overnight) was added. Neurons were fixed, and stained for MAP2c, synapsin, and with the Hoechst dye, and imaged. Note that red MAP2c staining also includes Dox's red fluorescence. (C) Synaptically developed primary cortical cultures at 28−32 DIV were pretreated with 5 mM Lev, and then a vehicle or with Dox (0.01 μM for 3 days, or 0.1 μM, overnight) was added. Neurons were then fixed, and stained with antibodies against γH2A.X and MAP2c, and with the Hoechst dye. Blue staining was used by the algorithm to identify and analyze γH2A.X.
S1813	Amlodipine Besylate Amlodipine Besylate is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.	Cell Discov, 2020, 6(1):96 Oncogene, 2019, 38(1):120-139
S1293	Cilnidipine Cilnidipine (FRC-8653) is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96 Res Sq, 2020, rs.3.rs-48659
S1811	Amiloride HCl Amiloride is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).	Signal Transduct Target Ther, 2020, 5(1):214 PLoS Genet, 2020, 16(10):e1009100 Drug Discov Ther, 2020, 14(5):256-258
S6920^新	SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S3242^新	Loureirin B Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the K_ATP current, influx of Ca²⁺ to the intracellular.
S6847^新	ML-9 HCl ML-9 HCl (ML-9 hydrochloride) is a selective and potent inhibitor of Akt kinase, myosin light chain kinase (MLCK) and stromal interaction molecule 1 (STIM1). ML-9 HCl is also a potent inhibitor of Ca2+-permeable channels. ML-9 HCl is a lysosomotropic agent targeting autophagy and cell death.	J Mol Endocrinol, 2019, 63(3):199-213
S6834^新	CM 4620 CM 4620 is an inhibitor of calcium-release activated calcium-channel (CRAC channel). CM4620 inhibits Orai1/STIM1-mediated Ca2+ currents and Orai2/STIM1-mediated currents with IC50 of near 120 nM and 900 nM, respectively.
S0016^新	SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S0000^新	Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 0.001 μM.
S1425	Ranolazine 2HCl Ranolazine 2HCl (RS-43285) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.	Front Pharmacol, 2019, 10:1367
S4202	Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.	Nat Commun, 2019, 10(1):3838 Clin Cancer Res, 2019, clincanres.1768.2019 EBioMedicine, 2019, 48:70-80	The proportion of SP cells in HepG2 and HCCLM3 cell lines were 0.16% and 32.2%, which reduced to 0% and 0.28% in the presence of verapamil.
S2482	Manidipine 2HCl Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.		Manidipine decreases the accumulation of HCMV Early and Late proteins. HFFs were infected with HCMV AD169 and then treated with test compounds or DMSO as a control. NTZ-treated samples were also included as a control for inhibition of E and L protein expression. At the indicated times p.i., total cell extracts were prepared and analyzed by WB with anti-IEA, anti-UL44, and anti-UL99 antibodies. Tubulin immunodetection served as a loading control. Images are representative of three independent experiments.
S1799	Ranolazine Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
S1662	Isradipine Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.	Cell Discov, 2020, 6(1):96 Drug Metab Dispos, 2015, 43(12):1934-7
S1905	Amlodipine Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.	ACS Infect Dis, 2020, acsinfecdis.0c00486 J Med Toxicol, 2020, 16(1):61-66 Oncogene, 2019, 38(1):120-139
S1885	Felodipine Felodipine (CGH-869) is a selective L-type Ca²⁺ channel blocker with IC50 of 0.15 nM.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96
S2481	Manidipine Manidipine is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive.	Antiviral Res, 2018, 150:130-136
S1748	Nisoldipine Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Ca_v1.2 with IC50 of 10 nM.	Cell Discov, 2020, 6(1):96 bioRxiv, 2020, 2020/9/20.4.7.30734
S1747	Nimodipine Nimodipine (BAY E 9736) is a dihydropyridine calcium channel blocker and an autophagy inhibitor, used in the treatment of high blood pressure.	Cell Discov, 2020, 6(1):96 G3 (Bethesda), 2020, 4;10(5):1585-1597 Antiviral Res, 2016, 132:38-45	Assessment of the role of Ca2+ channels during RSV replication. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with calcium channel blockers nifedipine, nimodipine, and tetrandrine (A), at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. NS, no differences at a significance level of 0.05.
S2721	Nilvadipine Nilvadipine (ARC029, FR34235) is a potent calcium channel blocker with an IC50 of 0.03 nM.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1994	Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
S2114	Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).	Cell Syst, 2019, 8(2):97-108 Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
S4181	Nicardipine HCl Nicardipine HCl (RS-69216) is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96
S1808	Nifedipine Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.	Cell Discov, 2020, 6(1):96 Front Pharmacol, 2019, 10:381 Biochem Biophys Res Commun, 2019, 509(1):76-81	The fold change of C-peptide content after octreotide, nicorandil and nifedipine treatment. Octreotide, nicorandil and nifedipine decreased insulin secretion in wild-type, heterozygous mutated and homozygous mutated cells.
S2080	Clevidipine Butyrate Clevidipine Butyrate is a dihydropyridine calcium channel blocker, uses as an agent for the reduction of blood pressure.	ACS Infect Dis, 2020, acsinfecdis.0c00486
S2017	Benidipine HCl Benidipine HCl (KW-3049) is a hydrochloride salt form of benidipine which is a dihydropyridine calcium channel blocker.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Cell Discov, 2020, 6(1):96 Life Sci, 2019, 227:74-81
S2030	Flunarizine 2HCl Flunarizine 2HCl (KW-3149, R14950) is a dihydrochloride salt form which is a calcium channel blocker with a K_i of 68 nM.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S2491	Nitrendipine Nitrendipine (Bayotensin) is a dihydropyridine calcium channel blocker with an IC50 of 95 nM.
S3053	Azelnidipine Azelnidipine (UR-12592) is a dihydropyridine calcium channel blocker.
S2573	Tetracaine HCl Tetracaine HCl (Amethocalne) is a hydrochloride salt form of tetracaine which is a potent local anaesthetic and a channel function allosteric inhibitor.
S1865	Diltiazem HCl Diltiazem (Tiazac, RG 83606) HCl is a benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions.	J Cell Mol Med, 2018, 22(12):5964-5977 FASEB J, 2017, 31(2):625-635	Gentisic acid reduces interstitial and perivascular fibrosis in mice with transverse aortic constriction (TAC). Representative images of Masson's trichrome staining of the hearts of mice in the sham and TAC + vehicle, gentisic acid, bisoprolol, or diltiazem groups. Scale bar = 50 μm. A, Interstitial fibrosis and B, perivascular fibrosis are shown. Fibrotic areas are stained blue.
S3045	Cinepazide maleate Cinepazide maleate is a maleate salt form of cinepazide which is a vasodilator.
S5255	Nicardipine Nicardipine is a potent calcium channel blockader with marked vasodilator action.
S8380	YM-58483 (BTP2) YM-58483/BTP2 is a blocker of store-operated Ca2+ entry (SOCE), which regulates the activation of non-excitable cells such as lymphocytes.	Cell Stem Cell, 2018, 22(6):865-878
S6657	2-Aminoethyl Diphenylborinate (2-APB) 2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulate IP3-induced calcium release.2-APB also inhibits the SOC channel activity and activates TRP channel at higher concentrations.	Cell Discov, 2020, 6(1):96
S4626	Ethosuximide Ethosuximide is a succinimide anticonvulsant, used mainly in absence seizures; A calcium channel blocker.	Nature, 2018, 554(7692):317-322	Antidepressant effects caused by systemic ethosuximide injection (200 mg kg−1, i.p.; c, d) in the FST(forced swim test) and SPT (sucrose preference test) 1 h after treatment.
S4597	Lercanidipine hydrochloride Lercanidipine is a calcium channel blocker of the dihydropyridine class.	J Phys Chem B, 2013, 117(23):6868-73
S4977	Efonidipine Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
S5279	Fendiline hydrochloride Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras.
S3845	Panaxadiol Panaxadiol (20(R)-Panaxadiol) is a triterpene sapogenin originally found in species of Panax (ginseng) and exhibits anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities. It inhibits Ca2+ channels, decreasing channel open time and open state probability in vitro and displaying anti-arrhythmic potential.
S3700	DHBP dibromide DHBP (1,1'-diheptyl-4,4'-bipyridinium), a viologen for electrochromic memory display agent, inhibits the calcium release induced by 2 mM caffeine and 2 μg/ml polylysine with an IC50 value of 5 μg/ml and 4 μg/ml respectively.
S2403	Tetrandrine Tetrandrine (Fanchinine), a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a calcium channel blocker.	Nat Commun, 2020, 27;11(1):1620 Ann Transl Med, 2020, 8(16):1018 Cell Death Dis, 2019, 10(2):38	BMMs were seeded in a collage I-coated plate and incubated with RANKL (100 ng/ml) and M-CSF (50 ng/ml) for 5 d. When mature osteoclasts were observed, they were digested by collagenase and seeded on bovine bone slices. The bone slices were treated with or without tetrandrine for an additional 2 d. Then, the cells were stained with rhodamine–phalloidin to observe the F-actin rings, and the areas of F-actin rings were calculated by Image-Pro Plus 6.0 software.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S3931	Ginsenoside Rd Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
S5514	Lanthanum(III) chloride heptahydrate Lanthanum(III) chloride is the inorganic compound used in biochemical research to block the activity of divalent cation channels, mainly calcium channels.
S3766	Tanshinone IIA sulfonate sodium Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
S4084	Lomerizine 2HCl Lomerizine dihydrochloride (KB-2796) is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
S4648	Dantrolene sodium hemiheptahydrate Dantrolene sodium hemiheptahydrate (Dantrium) ia a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber.
S3682	Ethyl 3-Aminobenzoate methanesulfonate Ethyl 3-Aminobenzoate (Ethyl m-Aminobenzoate, NSC 93790, Tricaine) can block the generation of action potentials via voltage-dependent Na+-channels and usually used for anesthesia, sedation, or euthanasia of fish.
S9400	Rhynchophylline Rhynchophylline (Mitrinermine), an active component isolated from species of the genus Uncaria, acts as a calcium channel blocker and is widely used in traditional Chinese medicine mainly for treating ailments of central nervous and cardiovascular systems, such as lightheadedness, convulsions, numbness, and hypertension.
S3674	Levamlodipine Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.
S3883	Protopine Protopine (Corydinine, Fumarine, Biflorine, Macleyine), an alkaloid present in different plants, has been shown to exhibit a number of activities, such as inhibition of calcium influx through both voltage and receptor-operated channels and inhibition of rabbit blood platelet aggregation. It also possesses anti-cholinergic and anti-histaminic as well as anti-bacterial activities.
S5567	Trimethadione Trimethadione is an oxazolidinedione anticonvulsant and often used to treat epileptic conditions that are resistant to other treatments.
S9566	Bepridil hydrochloride Bepridil hydrochloride is an anti-anginal drug classified as a calcium channel blocker. It also blocks multiple other ion channels, including sodium and potassium channels.
S6473	Pinaverium bromide Pinaverium bromide (Icosapentaenoic acid) acts as a calcium channel blocker and is useful for functional gastrointestinal disorders.
S4727	Cinnarizine Cinnarizine (Stugeron, Dimitronal, Stutgin, Cinarizine) is a medication derivative of piperazine, and characterized as an antihistamine and a calcium channel blocker.

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S2050	Strontium Ranelate Strontium Ranelate is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.
S7924	Bay K 8644 Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.	J Cell Physiol, 2018, 10.1002/jcp.27791	Western blot analysis of myocardium lysate at 4 weeks. Hypertrophic markers were tested in mouse cardiomyocyte cell line HL-1 Bay-K-8644.
S4209	Chlorocresol Chlorocresol is an activator of ryanodine receptor.

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S2050

Strontium Ranelate

Strontium Ranelate is a strontium(II) salt of ranelic acid for (-)-desmethoxyverapamil binding to calcium channel with IC50 of 0.5 mM.

S7924

Bay K 8644

Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.

J Cell Physiol, 2018, 10.1002/jcp.27791

S4209

Chlorocresol

Chlorocresol is an activator of ryanodine receptor.

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S0870^新	Barnidipine Barnidipine (Libradin, Mepirodipine, Vasexten, YM-09730-5, Cyress, Hypoca, Oldeca) is an antihypertensive drug that belongs to the dihydropyridine (DHP) group of calcium antagonist (CaA) with Ki of 0.21 nM for [³H]nitrendipine binding sites.
S2436^新	Pranidipine Pranidipine is a new 1,4-dihydropyridine calcium channel blocker. Pranidipine can enhance cyclic GMP-independent nitric oxide-induced relaxation of the rat aorta.
S4931	Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
S3809	Imperatorin Imperatorin (Ammidin, Marmelosin, Pentosalen, 8-Isoamylenoxypsoralen), a naturally occurring psoralen-type furanocoumarin, is a potent myorelaxant agent and acts as a calcium antagonist on vascular smooth muscle.	Adv Sci (Weinh), 2020, 7(16):2000925 Theriogenology, 2019, 10.1016/j.theriogenology
S2953	Dooku1 Dooku1 is an analog of Yoda1 with antagonist activity against mechanosensitive Piezo1 channel. Dooku1 inhibits 2 μM Yoda1-induced Ca²⁺-entry with IC50 of 1.3 μM in HEK 293 cells and 1.5 μM in HUVECs, respectively.
S5861	Lercanidipine Lercanidipine is a vasoselective dihydropyridine calcium antagonist used for the treatment of essential hypertension.

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S9151	Praeruptorin E Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.

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S9151

Praeruptorin E

Praeruptorin E, isolated from Peucedanum praeruptorum Dunn., is a cardiotonic agent with selective cardiac calcium channel agonistic effect.

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S3236^新	Mesaconitine Mesaconitine, one of the aconite alkaloids in Aconiti tuber, increases the [Ca2+]i level in endothelial cells by influx of Ca2+ from extracellular spaces.
S0973^新	Wilforgine Wilforgine, one of the major bioactive sesquiterpene alkaloids in Tripterygium wilfordii Hook. F., induces microstructural and ultrastructural changes in the muscles of M. separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
S2535	Econazole nitrate Econazole Nitrate (NSC 243115) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.	Biomol Ther (Seoul), 2020, 25
S2415	Astragaloside A Astragaloside A (Astragaloside IV) is the primary pure saponin isolated from Astragalus membranaceus, which has been widely used for the treatment of cardiovascular diseases.	Carcinogenesis, 2020, 41(7):993-1004 J Med Virol, 2019, 91(8):1440-1447
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

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S2446	Levosimendan Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.	Antiviral Res, 2017, 146:76-85	(B-E) The % of GFP-positive cells upon compound treatment were determined for the indicated HIV-1 latency cell lines (B. J-LAT 6.3; C. JLAT 10.6; D. CA5; E. EF7). Results were normalized to DMSO control. Values represent the mean ± s.d. (n = 4-6). * p < 0.05, one-way ANOVA followed by Tukey’s multiplecomparison test
S1911	Disodium Cromoglycate Disodium Cromoglycate (FPL 670, Cromolyn) is an antiallergic drug with IC50 of 39 μg/mL.
S5478	Dantrolene sodium Dantrolene sodium acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.	Sci Rep, 2019, 9(1):3487

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S2446

Levosimendan

Levosimendan is a calcium sensitizer acting through calcium-dependent binding to cardiac troponin C (cTnC), provides treatment for heart failure.

Antiviral Res, 2017, 146:76-85

S1911

Disodium Cromoglycate

Disodium Cromoglycate (FPL 670, Cromolyn) is an antiallergic drug with IC50 of 39 μg/mL.

S5478

Dantrolene sodium

Dantrolene sodium acts as a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

Sci Rep, 2019, 9(1):3487

研究分野別

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カルシウムチャネル

シグナル伝達経路

研究分野

阻害剤の選択性比較

Calcium Channel製品