カリウムチャネル

信号経路図

研究分野

阻害剤の選択性比較
溶解度

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
S4733	Retigabine	<1 mg/mL	60 mg/mL	35 mg/mL
S4734	Retigabine 2HCl	75 mg/mL	75 mg/mL	25 mg/mL
S1426	Repaglinide	<1 mg/mL	91 mg/mL	91 mg/mL
S1971	Nicorandil	17 mg/mL	42 mg/mL	42 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
S3151	Gliquidone	<1 mg/mL	105 mg/mL	6 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
S2562	Hydralazine HCl	1 mg/mL	<1 mg/mL	<1 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
S4630	Diazoxide	<1 mg/mL	46 mg/mL	<1 mg/mL
S4632	Hexachlorophene	<1 mg/mL	81 mg/mL	81 mg/mL
S2073	Mitiglinide Calcium	<1 mg/mL	<1 mg/mL	2 mg/mL

Potassium Channel阻害剤(16)
Potassium Channel活性剤(6)
Potassium Channel拮抗剤(1)
新Potassium Channel製品

製品コード	製品説明	文献中の使用例	お客様のフィードバック
S1658	Dofetilide Dofetilide(Tikosyn) is a class III antiarrhythmic agent.	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 nward-rectifying K+ currents and time-independent outward currents	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Virol J, 2016, 13:25	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は一種のsodium/potassium-ATPase阻害剤で、同時に一種の自食活性剤ですが、各種の心臓律動異常の治療に使用されます。	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 medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.		(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.
S1426	Repaglinide Repaglinide is for the treatment of type II diabetes.
S2502	Quinine HCl Dihydrate Quinine hydrochloride dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.
S1716	Glyburide (Glibenclamide) Glyburide (Glibenclamide) is an anti-diabetic compound in a class of medications known as sulfonylureas, closely related to sulfa agents.
S2443	Tolbutamide タイプ2糖尿病を治療するために、トルブタミドがダイエットと運動とともに、そして、時々他の薬物で使われます
S2114	Dronedarone HCl Dronedarone HCl is a therapy for the treatment of patients with paroxysmal and persistent atrial fibrillation or atrial flutter.		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.
S8016	Vonoprazan Fumarate (TAK-438) Vonoprazan Fumarate (TAK-438)は、抗分泌性新しいカリウム競争的酸性のブロッカー（P-CAB）タイプですエージェント、可逆的に胃H⁺、K⁺-ATPaseを妨げます。IC50 が 19 nM 、 pH 6.5です。
S2825	ML133 HCl ML133 HCl is a potent potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5).
S2601	Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 ¡À 30 nM
S4037	Doxapram HCl Doxapram HClはTASK-1, TASK-3, TASK-1/TASK-3 のヘテロチャネル機能を阻害、 EC50 がそれぞれ410 nM、 37 μM、 9 μMです。
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.
S3151	Gliquidone Gliquidone is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.
S4733^新	Retigabine
S4734^新	Retigabine 2HCl
S1971	Nicorandil Nicorandil is potassium channel activator.	J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477 Sci Rep, 2017, 7(1):3156	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 hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.	Xenobiotica, 2014, 44(9):827-41
S4630	Diazoxide
S4632	Hexachlorophene

製品コード	製品説明	文献中の使用例	お客様のフィードバック
S1658	Dofetilide Dofetilide(Tikosyn) is a class III antiarrhythmic agent.	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 nward-rectifying K+ currents and time-independent outward currents	Antimicrob Agents Chemother, 2014, 58(8):4875-84 Virol J, 2016, 13:25	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は一種のsodium/potassium-ATPase阻害剤で、同時に一種の自食活性剤ですが、各種の心臓律動異常の治療に使用されます。	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 medium-to-long acting sulfonylurea anti-diabetic compound with an ED50 of 182 μg/kg.		(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.
S1426	Repaglinide Repaglinide is for the treatment of type II diabetes.
S2502	Quinine HCl Dihydrate Quinine hydrochloride dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.
S1716	Glyburide (Glibenclamide) Glyburide (Glibenclamide) is an anti-diabetic compound in a class of medications known as sulfonylureas, closely related to sulfa agents.
S2443	Tolbutamide タイプ2糖尿病を治療するために、トルブタミドがダイエットと運動とともに、そして、時々他の薬物で使われます
S2114	Dronedarone HCl Dronedarone HCl is a therapy for the treatment of patients with paroxysmal and persistent atrial fibrillation or atrial flutter.		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.
S8016	Vonoprazan Fumarate (TAK-438) Vonoprazan Fumarate (TAK-438)は、抗分泌性新しいカリウム競争的酸性のブロッカー（P-CAB）タイプですエージェント、可逆的に胃H⁺、K⁺-ATPaseを妨げます。IC50 が 19 nM 、 pH 6.5です。
S2825	ML133 HCl ML133 HCl is a potent potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5).
S2601	Gliclazide Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 ¡À 30 nM
S4037	Doxapram HCl Doxapram HClはTASK-1, TASK-3, TASK-1/TASK-3 のヘテロチャネル機能を阻害、 EC50 がそれぞれ410 nM、 37 μM、 9 μMです。
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	文献中の使用例	お客様のフィードバック
S4733^新	Retigabine
S4734^新	Retigabine 2HCl
S1971	Nicorandil Nicorandil is potassium channel activator.	J Cardiovasc Pharmacol Ther, 2016, 10.1177/1074248416636477 Sci Rep, 2017, 7(1):3156	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 hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.	Xenobiotica, 2014, 44(9):827-41
S4630	Diazoxide
S4632	Hexachlorophene

製品コード	製品説明	文献中の使用例	お客様のフィードバック
S3151	Gliquidone Gliquidone is an ATP-sensitive K⁺ channel antagonist with IC50 of 27.2 nM.

製品コード

製品説明

文献中の使用例

お客様のフィードバック

S3151

Gliquidone

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

研究分野別

製品類型

カリウムチャネル

信号経路図

研究分野