カリウムチャネル

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
S1658	Dofetilide	<1 mg/mL	88 mg/mL	<1 mg/mL
S2456	Chlorpromazine HCl	71 mg/mL	71 mg/mL	71 mg/mL
S1979	Amiodarone HCl	<1 mg/mL	23 mg/mL	11 mg/mL
S1344	Glimepiride	<1 mg/mL	11 mg/mL	<1 mg/mL
S1160	TRAM-34	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S3242	Loureirin B	-1 mg/mL	100 mg/mL	-1 mg/mL
S0524	A2793	<1 mg/mL	53 mg/mL	25 mg/mL
S0467	Emodepside	<1 mg/mL	100 mg/mL	20 mg/mL
S0188	GSK369796 Dihydrochloride	40 mg/mL	86 mg/mL	10 mg/mL
S4353	Terfenadine	<1 mg/mL	94 mg/mL	27 mg/mL
S6627	E-4031 dihydrochloride	48 mg/mL	30 mg/mL	<1 mg/mL
S1426	Repaglinide	<1 mg/mL	91 mg/mL	91 mg/mL
S2502	Quinine HCl Dihydrate	43 mg/mL	79 mg/mL	79 mg/mL
S1716	Glyburide (Glibenclamide)	<1 mg/mL	99 mg/mL	<1 mg/mL
S2443	Tolbutamide	<1 mg/mL	54 mg/mL	54 mg/mL
S2114	Dronedarone HCl	<1 mg/mL	80 mg/mL	40 mg/mL
S2489	Nateglinide	<1 mg/mL	63 mg/mL	63 mg/mL
S8016	Vonoprazan Fumarate (TAK-438)	<1 mg/mL	62 mg/mL	<1 mg/mL
S2825	ML133 HCl	<1 mg/mL	63 mg/mL	6 mg/mL
S2601	Gliclazide	<1 mg/mL	65 mg/mL	<1 mg/mL
S1715	Glipizide	<1 mg/mL	89 mg/mL	<1 mg/mL
S6284	Tetraethylammonium bromide	-1 mg/mL	42 mg/mL	-1 mg/mL
S9223	Talatisamine	-1 mg/mL	35 mg/mL	-1 mg/mL
S5371	Ajmaline	-1 mg/mL	65 mg/mL	-1 mg/mL
S5257	Doxapram	<1 mg/mL	75 mg/mL	75 mg/mL
S4037	Doxapram HCl	25 mg/mL	87 mg/mL	2 mg/mL
S9251	Oxypeucedanin	-1 mg/mL	24 mg/mL	-1 mg/mL
S4583	Butamben	38 mg/mL	38 mg/mL	38 mg/mL
S6554	ML365	<1 mg/mL	72 mg/mL	18 mg/mL
S4186	Domiphen Bromide	83 mg/mL	83 mg/mL	83 mg/mL
S2405	Sophocarpine	6 mg/mL	49 mg/mL	49 mg/mL
S5028	4-Aminopyridine	-1 mg/mL	18 mg/mL	-1 mg/mL
S8615	Sodium dichloroacetate (DCA)	30 mg/mL	30 mg/mL	30 mg/mL
S5773	NS1643	˂1 mg/mL	76 mg/mL	76 mg/mL
S2073	Mitiglinide Calcium	<1 mg/mL	<1 mg/mL	2 mg/mL
S5749	Chlorpromazine	-1 mg/mL	64 mg/mL	-1 mg/mL
S6559	ML-297	<1 mg/mL	66 mg/mL	15 mg/mL
S0462	NS-1619	˂1 mg/mL	72 mg/mL	72 mg/mL
S0144	ICA 069673	<1 mg/mL	54 mg/mL	54 mg/mL
S1971	Nicorandil	17 mg/mL	42 mg/mL	42 mg/mL
S1383	Minoxidil	<1 mg/mL	0.25 mg/mL	<1 mg/mL
S2562	Hydralazine HCl	1 mg/mL	<1 mg/mL	<1 mg/mL
S4630	Diazoxide	<1 mg/mL	46 mg/mL	<1 mg/mL
S4733	Retigabine	<1 mg/mL	60 mg/mL	35 mg/mL
S4632	Hexachlorophene	<1 mg/mL	81 mg/mL	81 mg/mL
S4734	Retigabine 2HCl	75 mg/mL	75 mg/mL	25 mg/mL
S6572	ML335	<1 mg/mL	75 mg/mL	5 mg/mL
S0476	SCH-23390 hydrochloride	20 mg/mL	65 mg/mL	25 mg/mL
S0398	Astemizole	<1 mg/mL	92 mg/mL	9 mg/mL
S3151	Gliquidone	<1 mg/mL	105 mg/mL	6 mg/mL
S0075	ICA-110381	<1 mg/mL	53 mg/mL	4 mg/mL

Potassium Channel製品

All (51) Potassium Channel阻害剤(36) Potassium Channel活性剤(11) Potassium Channel拮抗剤(3) Potassium Channelモジュレータ(1)

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
S1658	Dofetilide Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.	PLoS Pathog, 2020, 16;16(3):e1008341 Toxicol In Vitro, 2020, 104928 Clin Transl Sci, 2019, 12(6):687-697
S2456	Chlorpromazine HCl Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.	Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734 J Virol, 2018, 92(24)	Low-micromolar amounts of chlorpromazine inhibit SARS-CoV-induced cytopathology. Vero E6 cells in 96-well plates were infected with SARS-CoV isolate Frankfurt-1 (MOI, 0.005) in the presence of 0 to 16 μM CPZ (B), given at t of +1 h p.i. Cells were incubated for 3 days, and viability was monitored using an MTS assay. In parallel, potential compound cytotoxicity was monitored in mock-infected Vero E6 cells. Graphs show the results (averages and SD) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the EC50, CC50, and SI values are given.
S1979	Amiodarone HCl Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.	Drug Metab Dispos, 2020, 48(8):613-621 Cell Syst, 2019, 8(2):97-108 Gynecol Oncol, 2018, 151(3):525-532	Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. P<0.05, P<0.01, and **P<0.0001.
S1344	Glimepiride Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.	Sci Rep, 2017, 7(1):3156	(E) ELISA analysis for C-peptide levels in the presence of vehicle, diazoxide and glimepiride. (F) The fold change of C-peptide content after diazoxide and glimepiride stimulation. Diazoxide and glimepiride decreased and increased C-peptide secretion in wild-type and heterozygous mutated cells, respectively. Neither diazoxide nor glimepiride had an effect on homozygous mutated cells.
S1160	TRAM-34 TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with K_d of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450.	Am J Cancer Res, 2020, 10(10):3302-3315
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.
S0524^新	A2793 A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.
S0467^新	Emodepside Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.
S0188^新	GSK369796 Dihydrochloride GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.
S4353^新	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.
S6627^新	E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.
S1426	Repaglinide Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.	Drug Metab Dispos, 2019, ;47(3):215-226
S2502	Quinine HCl Dihydrate Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.
S1716	Glyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.	Am J Transplant, 2020, 10.1111/ajt.16071
S2443	Tolbutamide Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8
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 (*).
S2489	Nateglinide Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.	Cell Syst, 2019, 8(2):97-108 Nature, 2018, 560(7718):372-376
S8016	Vonoprazan Fumarate (TAK-438) Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.
S2825	ML133 HCl ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.	Mol Pain, 2019, 15:1744806919838947 Neurosci Bull, 2018, 10.1007/s12264-018-0285-8
S2601	Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
S1715	Glipizide Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
S6284	Tetraethylammonium bromide Tetraethylammonium bromide is used as the source of tetraethylammonium ions in pharmacological and physiological studies, but is also used in organic chemical synthesis. It blocks selective potassium channels.
S9223	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S5371	Ajmaline Ajmaline, found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.
S5257	Doxapram Doxapram is a central respiratory stimulant with a brief duration of action.	Biomed Chromatogr, 2018, 32(10)
S4037	Doxapram HCl Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
S9251	Oxypeucedanin Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.
S4583	Butamben Butamben is a long-duration local anesthetic used for the treatment of chronic pain.
S6554	ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S4186	Domiphen Bromide Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.
S2405	Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.	Int J Biol Sci, 2019, 15(11):2497-2508 Front Pharmacol, 2019, 10:1219 Br J Pharmacol, 2018, 175(6):859-876
S5028	4-Aminopyridine 4-Aminopyridine (4-AP) is a potent and non-selective inhibitor of voltage gated potassium channels (Kv) with IC50 values of 170 μM and 230 μM for Kv1.1 and Kv1.2 in CHO cells, respectively.
S8615	Sodium dichloroacetate (DCA) Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na⁺-K⁺-2Cl^- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
S5773	NS1643 NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.
S2073	Mitiglinide Calcium Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
S5749	Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.	Biomaterials, 2020, 232:119701 Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734
S6559^新	ML-297 ML-297 is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.
S0462^新	NS-1619 NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.
S0144^新	ICA 069673 ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.
S1971	Nicorandil Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).	Sci Rep, 2017, 7(1):3156 J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477	Concentration-dependent effects of nicorandil to protect against stress and recovery (S/R)-induced cell injury and reactive oxygen species (ROS) production in nonaffected induced pluripotent stem cell (iPSC)-derived cardiomyocytes. The N-iCMs were subjected to 2 hours of oxidative stress followed by recovery. Protective effects of different concentrations of nicorandil (0.1, 1, 10, and 100 μmol/L) on cell injury and ROS production were assessed after 4 hours of recovery by measuring lactate dehydrogenase (LDH) release into the supernatant and evaluating dihydroethidium (DHE) fluorescent intensity, respectively. A, Stress induces an increase in LDH release in N-iCMs, which is mitigated by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. B, Stress induced an increase in ROS levels as indicated by DHE fluorescence, which is abolished by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. Data are mean ± standard error of the mean (SEM) of values from 3 independent experiments (n = 3/group). *P ≤ .05 versus control.
S1383	Minoxidil Minoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth.	Oncotarget, 2016, 7(43):69703-69717	Effect of Rhiz in combination with potassium channel openers Minox (A) on viability of PC-3 and DU145 cells. Cells were co-treated with indicated concentrations of the drugs for 48 h. Cell viability was measured by MTT assay.
S2562	Hydralazine HCl Hydralazine HCl is a hydrochloride salt of hydralazine, which is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles.	Biogerontology, 2016, 17(5-6):907-920 Xenobiotica, 2014, 44(9):827-41
S4630	Diazoxide Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.	Free Radic Biol Med, 2017, 112:616-630
S4733	Retigabine Retigabine (D-23129) is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.	J Neurosci, 2020, 40(34):6522-6535 Hear Res, 2020, 388:107884 Mol Pain, 2018, 14:1744806918793229
S4632	Hexachlorophene Hexachlorophene (Hexachlorofen, Fostril, Nabac, pHisoHex) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; It can also attenuate Wnt/beta-catenin signaling through the Siah-1-mediated beta-catenin degradation.	Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
S4734	Retigabine 2HCl Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.	J Neurosci, 2020, 40(34):6522-6535 Mol Pain, 2018, 14:1744806918793229
S6572	ML335 ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
S0476^新	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S0398^新	Astemizole Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S3151	Gliquidone Gliquidone (Glurenorm) is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.	Front Cell Dev Biol, 2020, 8:269 Drug Test Anal, 2018, 10(3):609-617
S0075^新	ICA-110381 ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

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
S1658	Dofetilide Dofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.	PLoS Pathog, 2020, 16;16(3):e1008341 Toxicol In Vitro, 2020, 104928 Clin Transl Sci, 2019, 12(6):687-697
S2456	Chlorpromazine HCl Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.	Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734 J Virol, 2018, 92(24)	Low-micromolar amounts of chlorpromazine inhibit SARS-CoV-induced cytopathology. Vero E6 cells in 96-well plates were infected with SARS-CoV isolate Frankfurt-1 (MOI, 0.005) in the presence of 0 to 16 μM CPZ (B), given at t of +1 h p.i. Cells were incubated for 3 days, and viability was monitored using an MTS assay. In parallel, potential compound cytotoxicity was monitored in mock-infected Vero E6 cells. Graphs show the results (averages and SD) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the EC50, CC50, and SI values are given.
S1979	Amiodarone HCl Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias.	Drug Metab Dispos, 2020, 48(8):613-621 Cell Syst, 2019, 8(2):97-108 Gynecol Oncol, 2018, 151(3):525-532	Drugs across therapeutic indications induce lipid formation in hiPS-CM. Lipid accumulation was detected in cardiac cells using the LipidTox plate-based fluorescent assay on the Thermo Scientific CellInsight High Content platform. A) Ten drugs increased lipid levels in hiPS-CM following 48 h treatment. The lowest drug dose that induced a N1.5-fold increase in lipid formation is shown. B) Representative images (20×) from the assay are shown to the right. All drugs had >55% cell viability at 48 h at these tested concentrations. C) Of these 10 drugs, 8 significantly increased lipid accumulation following only 24 h treatment (images not shown). All drugs had >80% cell viability at 24 h at these drug doses. The graphs represent the mean fold-change of the lowest concentration of drug that significantly induced lipid formation >1.5-fold more than vehicle control. P<0.05, P<0.01, and **P<0.0001.
S1344	Glimepiride Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.	Sci Rep, 2017, 7(1):3156	(E) ELISA analysis for C-peptide levels in the presence of vehicle, diazoxide and glimepiride. (F) The fold change of C-peptide content after diazoxide and glimepiride stimulation. Diazoxide and glimepiride decreased and increased C-peptide secretion in wild-type and heterozygous mutated cells, respectively. Neither diazoxide nor glimepiride had an effect on homozygous mutated cells.
S1160	TRAM-34 TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with K_d of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450.	Am J Cancer Res, 2020, 10(10):3302-3315
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.
S0524^新	A2793 A2793 (Ethyl [(5-Chloroquinolin-8-yl)oxy]acetate) is an efficient inhibitor of TWIK-related spinal cord potassium channel (TRESK, K2P18, KCNK18) and TASK-1 (KCNK3) with IC50 of 6.8 μM for mouse TRESK.
S0467^新	Emodepside Emodepside (QHT06, BAY 44-4400, PF 1022-221), a semisynthetic derivative of PF1022A, is a cyclooctadepsipeptide with broad-spectrum anthelmintic activity. Emodepside activates Ca-dependent SLO-1-like K channels.
S0188^新	GSK369796 Dihydrochloride GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.
S4353^新	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.
S6627^新	E-4031 dihydrochloride E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type.
S1426	Repaglinide Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.	Drug Metab Dispos, 2019, ;47(3):215-226
S2502	Quinine HCl Dihydrate Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria.
S1716	Glyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.	Am J Transplant, 2020, 10.1111/ajt.16071
S2443	Tolbutamide Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8
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 (*).
S2489	Nateglinide Nateglinide (A-4166) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.	Cell Syst, 2019, 8(2):97-108 Nature, 2018, 560(7718):372-376
S8016	Vonoprazan Fumarate (TAK-438) Vonoprazan Fumarate (TAK-438) is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion. Phase 3.
S2825	ML133 HCl ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.	Mol Pain, 2019, 15:1744806919838947 Neurosci Bull, 2018, 10.1007/s12264-018-0285-8
S2601	Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
S1715	Glipizide Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
S6284	Tetraethylammonium bromide Tetraethylammonium bromide is used as the source of tetraethylammonium ions in pharmacological and physiological studies, but is also used in organic chemical synthesis. It blocks selective potassium channels.
S9223	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S5371	Ajmaline Ajmaline, found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent.
S5257	Doxapram Doxapram is a central respiratory stimulant with a brief duration of action.	Biomed Chromatogr, 2018, 32(10)
S4037	Doxapram HCl Doxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.
S9251	Oxypeucedanin Oxypeucedanin is a major coumarin aglycone that can be extracted from Ostericum koreanum. It is a kind of open-channel blocker of the hKv1.5 channel.
S4583	Butamben Butamben is a long-duration local anesthetic used for the treatment of chronic pain.
S6554	ML365 ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3).
S4186	Domiphen Bromide Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant.
S2405	Sophocarpine Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.	Int J Biol Sci, 2019, 15(11):2497-2508 Front Pharmacol, 2019, 10:1219 Br J Pharmacol, 2018, 175(6):859-876
S5028	4-Aminopyridine 4-Aminopyridine (4-AP) is a potent and non-selective inhibitor of voltage gated potassium channels (Kv) with IC50 values of 170 μM and 230 μM for Kv1.1 and Kv1.2 in CHO cells, respectively.
S8615	Sodium dichloroacetate (DCA) Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na⁺-K⁺-2Cl^- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.
S5773	NS1643 NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents.
S2073	Mitiglinide Calcium Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
S5749	Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.	Biomaterials, 2020, 232:119701 Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734

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S6559^新	ML-297 ML-297 is a potent and selective activator of Kir3.1/3.2 (G protein-coupled inwardly rectifying potassium, GIRK1/2) channel with EC50 of 0.16 μM and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML-297 is potential for the treatment of epilepsy.
S0462^新	NS-1619 NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels.
S0144^新	ICA 069673 ICA 069673 (compound 51) is an orally active, potent and selective KCNQ2/Q3 potassium channel activator with EC50 of 0.69 μM and 14.3 μM for KCNQ2/Q3 and KCNQ3/Q5, respectively.
S1971	Nicorandil Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).	Sci Rep, 2017, 7(1):3156 J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477	Concentration-dependent effects of nicorandil to protect against stress and recovery (S/R)-induced cell injury and reactive oxygen species (ROS) production in nonaffected induced pluripotent stem cell (iPSC)-derived cardiomyocytes. The N-iCMs were subjected to 2 hours of oxidative stress followed by recovery. Protective effects of different concentrations of nicorandil (0.1, 1, 10, and 100 μmol/L) on cell injury and ROS production were assessed after 4 hours of recovery by measuring lactate dehydrogenase (LDH) release into the supernatant and evaluating dihydroethidium (DHE) fluorescent intensity, respectively. A, Stress induces an increase in LDH release in N-iCMs, which is mitigated by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. B, Stress induced an increase in ROS levels as indicated by DHE fluorescence, which is abolished by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. Data are mean ± standard error of the mean (SEM) of values from 3 independent experiments (n = 3/group). *P ≤ .05 versus control.
S1383	Minoxidil Minoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth.	Oncotarget, 2016, 7(43):69703-69717	Effect of Rhiz in combination with potassium channel openers Minox (A) on viability of PC-3 and DU145 cells. Cells were co-treated with indicated concentrations of the drugs for 48 h. Cell viability was measured by MTT assay.
S2562	Hydralazine HCl Hydralazine HCl is a hydrochloride salt of hydralazine, which is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles.	Biogerontology, 2016, 17(5-6):907-920 Xenobiotica, 2014, 44(9):827-41
S4630	Diazoxide Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.	Free Radic Biol Med, 2017, 112:616-630
S4733	Retigabine Retigabine (D-23129) is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.	J Neurosci, 2020, 40(34):6522-6535 Hear Res, 2020, 388:107884 Mol Pain, 2018, 14:1744806918793229
S4632	Hexachlorophene Hexachlorophene (Hexachlorofen, Fostril, Nabac, pHisoHex) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; It can also attenuate Wnt/beta-catenin signaling through the Siah-1-mediated beta-catenin degradation.	Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
S4734	Retigabine 2HCl Retigabine is a novel anticonvulsant with activity in a broad range of seizure models. The mechanism of action involves opening of neuronal K(V)7.2-7.5 (formerly KCNQ2-5) voltage-activated K(+) channels.	J Neurosci, 2020, 40(34):6522-6535 Mol Pain, 2018, 14:1744806918793229
S6572	ML335 ML335 is a potent and selective TREK-1/2 activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.

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S0476^新	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S0398^新	Astemizole Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S3151	Gliquidone Gliquidone (Glurenorm) is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.	Front Cell Dev Biol, 2020, 8:269 Drug Test Anal, 2018, 10(3):609-617

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S0476^新

SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

S0398^新

Astemizole

Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.

S3151

Gliquidone

Gliquidone (Glurenorm) is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.

Front Cell Dev Biol, 2020, 8:269

Drug Test Anal, 2018, 10(3):609-617

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S0075^新	ICA-110381 ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

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S0075^新

ICA-110381

ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 exhibits KCNQ2/Q3 agonist activity with EC50 of 0.38 μM and KCNQ1 antagonist activity with IC50 of 15 μM, respectively.

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Potassium Channel製品