Potassium Channel
Potassium Channel Products
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1658 |
DofetilideDofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug. |
||
S2456 |
Chlorpromazine HClChlorpromazine 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. |
![]() ![]() 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 HClAmiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias. |
![]() ![]() 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 |
GlimepirideGlimepiride 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. |
![]() ![]() (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-34TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. |
||
S3242New |
Loureirin BLoureirin 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 KATP current, influx of Ca2+ to the intracellular. |
||
S0741New |
A2764 dihydrochlorideA2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception. |
||
S0524New |
A2793A2793 (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. |
||
S0467New |
EmodepsideEmodepside (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. |
||
S0188New |
GSK369796 DihydrochlorideGSK369796 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. |
||
S1426 |
RepaglinideRepaglinide (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. |
||
S2502 |
Quinine HCl DihydrateQuinine 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 |
TolbutamideTolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes. |
||
S2114 |
Dronedarone HClDronedarone 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). |
![]() ![]() 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 |
NateglinideNateglinide (A-4166) 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) 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 HClML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1. |
||
S2601 |
GliclazideGliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. |
||
S1715 |
GlipizideGlipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. |
||
S6284 |
Tetraethylammonium bromideTetraethylammonium 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 |
TalatisamineTalatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. |
||
S5371 |
AjmalineAjmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. |
||
S5257 |
DoxapramDoxapram is a central respiratory stimulant with a brief duration of action. Doxapram is a selective TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel inhibitor with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
||
S4037 |
Doxapram HClDoxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
||
S9251 |
OxypeucedaninOxypeucedanin 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 |
ButambenButamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain. |
||
S6554 |
ML365ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
||
S4186 |
Domiphen BromideDomiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant. |
||
S2405 |
SophocarpineSophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
||
S5028 |
4-Aminopyridine4-Aminopyridine (4-AP, Fampridine, Dalfampridine) 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)Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), 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 |
NS1643NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. |
||
S4353 |
TerfenadineTerfenadine 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. |
||
S2073 |
Mitiglinide CalciumMitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. |
||
S5749 |
ChlorpromazineChlorpromazine (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. |
||
S6627 |
E-4031 dihydrochlorideE-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
||
S6559New |
ML-297ML-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. |
||
S6553New |
ML213ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively. |
||
S0462New |
NS-1619NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
||
S0144New |
ICA 069673ICA 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 |
NicorandilNicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). |
![]() ![]() 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 |
MinoxidilMinoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth. Minoxidil is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. |
![]() ![]() 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 HClHydralazine 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. |
||
S4630 |
DiazoxideDiazoxide (Sch-6783, SRG-95213, Proglycem) 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. |
||
S4733 |
RetigabineRetigabine (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. |
||
S4632 |
HexachloropheneHexachlorophene (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. |
||
S4734 |
Retigabine 2HClRetigabine 2HCl (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. |
||
S6572 |
ML335ML335 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. |
||
S0476New |
SCH-23390 hydrochlorideSCH-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. |
||
S0398New |
AstemizoleAstemizole 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 |
GliquidoneGliquidone (Glurenorm) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
||
S0075New |
ICA-110381ICA 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. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S1658 |
DofetilideDofetilide (UK-68798) is a selective potassium channel ((hERG)) blocker, used as a Class III antiarrhythmic drug. |
||
S2456 |
Chlorpromazine HClChlorpromazine 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. |
![]() ![]() 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 HClAmiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias. |
![]() ![]() 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 |
GlimepirideGlimepiride 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. |
![]() ![]() (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-34TRAM-34 (Triarylmethane-34) is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. |
||
S3242New |
Loureirin BLoureirin 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 KATP current, influx of Ca2+ to the intracellular. |
||
S0741New |
A2764 dihydrochlorideA2764 dihydrochloride is a selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1) with IC50 of 11.8 μM for the activated mTRESK channel. A2764 dihydrochloride has the potential for probing the role of TRESK channel in migraine and nociception. |
||
S0524New |
A2793A2793 (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. |
||
S0467New |
EmodepsideEmodepside (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. |
||
S0188New |
GSK369796 DihydrochlorideGSK369796 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. |
||
S1426 |
RepaglinideRepaglinide (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. |
||
S2502 |
Quinine HCl DihydrateQuinine 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 |
TolbutamideTolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes. |
||
S2114 |
Dronedarone HClDronedarone 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). |
![]() ![]() 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 |
NateglinideNateglinide (A-4166) 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) 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 HClML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1. |
||
S2601 |
GliclazideGliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. |
||
S1715 |
GlipizideGlipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. |
||
S6284 |
Tetraethylammonium bromideTetraethylammonium 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 |
TalatisamineTalatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. |
||
S5371 |
AjmalineAjmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. |
||
S5257 |
DoxapramDoxapram is a central respiratory stimulant with a brief duration of action. Doxapram is a selective TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel inhibitor with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
||
S4037 |
Doxapram HClDoxapram HCl inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. |
||
S9251 |
OxypeucedaninOxypeucedanin 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 |
ButambenButamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain. |
||
S6554 |
ML365ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
||
S4186 |
Domiphen BromideDomiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant. |
||
S2405 |
SophocarpineSophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
||
S5028 |
4-Aminopyridine4-Aminopyridine (4-AP, Fampridine, Dalfampridine) 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)Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), 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 |
NS1643NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. |
||
S4353 |
TerfenadineTerfenadine 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. |
||
S2073 |
Mitiglinide CalciumMitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. |
||
S5749 |
ChlorpromazineChlorpromazine (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. |
||
S6627 |
E-4031 dihydrochlorideE-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S6559New |
ML-297ML-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. |
||
S6553New |
ML213ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively. |
||
S0462New |
NS-1619NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
||
S0144New |
ICA 069673ICA 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 |
NicorandilNicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). |
![]() ![]() 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 |
MinoxidilMinoxidil (U-10858) is a vasodilator medication known for its ability to slow or stop hair loss and promote hair regrowth. Minoxidil is an ATP-sensitive potassium (KATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. |
![]() ![]() 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 HClHydralazine 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. |
||
S4630 |
DiazoxideDiazoxide (Sch-6783, SRG-95213, Proglycem) 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. |
||
S4733 |
RetigabineRetigabine (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. |
||
S4632 |
HexachloropheneHexachlorophene (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. |
||
S4734 |
Retigabine 2HClRetigabine 2HCl (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. |
||
S6572 |
ML335ML335 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. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S0476New |
SCH-23390 hydrochlorideSCH-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. |
||
S0398New |
AstemizoleAstemizole 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 |
GliquidoneGliquidone (Glurenorm) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
S0075New |
ICA-110381ICA 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. |