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
S6554	ML365	<1 mg/mL	72 mg/mL	18 mg/mL
S5773	NS1643	˂1 mg/mL	76 mg/mL	76 mg/mL
S6284	Tetraethylammonium bromide	-1 mg/mL	42 mg/mL	-1 mg/mL
S9251	Oxypeucedanin	-1 mg/mL	24 mg/mL	-1 mg/mL
S9223	Talatisamine	-1 mg/mL	35 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
S4037	Doxapram HCl	25 mg/mL	87 mg/mL	2 mg/mL
S5028	4-Aminopyridine	-1 mg/mL	18 mg/mL	-1 mg/mL
S2073	Mitiglinide Calcium	<1 mg/mL	<1 mg/mL	2 mg/mL
S6572	ML335	<1 mg/mL	75 mg/mL	5 mg/mL
S1971	Nicorandil	17 mg/mL	42 mg/mL	42 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
S3151	Gliquidone	<1 mg/mL	105 mg/mL	6 mg/mL

Potassium Channel製品

All (30) Potassium Channel阻害剤(22) Potassium Channel活性剤(7) Potassium Channel拮抗剤(1) 新Potassium Channel製品

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 is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.	J Pharm Biomed Anal, 2019, 172:183-188 Toxicol Appl Pharmacol, 2015, 285(1):51-60
S2456	Chlorpromazine HCl Chlorpromazine HCl 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.	Fish Shellfish Immunol, 2018, 84:138-147 Acta Biomater, 2018, 71:49-60 J Pharm Sci, 2018, 10.1016/j.xphs.2018.10.011	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.	Gynecol Oncol, 2018, 151(3):525-532 Toxicol Appl Pharmacol, 2015, 285(1):51-60	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 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.
S6554^新	ML365
S5773^新	NS1643
S6284^新	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.
S9251^新	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.
S9223^新	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S1426	Repaglinide Repaglinide 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.
S2443	Tolbutamide Tolbutamide is an inhibitor of potassium channel, used for type II diabetes.
S2114	Dronedarone HCl Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).	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 is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.	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.	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.
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.
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.
S2073	Mitiglinide Calcium Mitiglinide Calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
S6572^新	ML335
S1971	Nicorandil Nicorandil 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.
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.	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(free base) 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.
S4632	Hexachlorophene Hexachlorophene 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.
S3151	Gliquidone Gliquidone is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.	Drug Test Anal, 2018, 10(3):609-617

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 is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug.	J Pharm Biomed Anal, 2019, 172:183-188 Toxicol Appl Pharmacol, 2015, 285(1):51-60
S2456	Chlorpromazine HCl Chlorpromazine HCl 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.	Fish Shellfish Immunol, 2018, 84:138-147 Acta Biomater, 2018, 71:49-60 J Pharm Sci, 2018, 10.1016/j.xphs.2018.10.011	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.	Gynecol Oncol, 2018, 151(3):525-532 Toxicol Appl Pharmacol, 2015, 285(1):51-60	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 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.
S6554^新	ML365
S5773^新	NS1643
S6284^新	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.
S9251^新	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.
S9223^新	Talatisamine Talatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities.
S1426	Repaglinide Repaglinide 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.
S2443	Tolbutamide Tolbutamide is an inhibitor of potassium channel, used for type II diabetes.
S2114	Dronedarone HCl Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).	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 is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.	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.	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.
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.
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.
S2073	Mitiglinide Calcium Mitiglinide Calcium is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

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
S6572^新	ML335
S1971	Nicorandil Nicorandil 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.
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.	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(free base) 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.
S4632	Hexachlorophene Hexachlorophene 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.