Potassium Channel
Inhibitory Selectivity
Potassium Channel Products
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
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. |
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S4489 |
Tetraethylammonium chlorideTetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties. |
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S4495 |
QuinineQuinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM. |
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S4681 |
Quinidine hydrochloride monohydrateQuinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM. |
||
S9223 |
TalatisamineTalatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. |
||
E0144New |
Vernakalant (RSD1235) HydrochlorideVernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period. |
||
E0015New |
IberiotoxinIberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM. |
||
E0012New |
1-EBIO1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells. |
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E0001New |
DCPIBDCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM. |
||
S0524 |
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. |
||
S3242 |
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. |
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S0741 |
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. |
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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. |
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S0087 |
JNJ 303JNJ 303 is a potent blocker of the voltage dependent IKs-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP). |
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S6554 |
ML365ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
||
S2405 |
SophocarpineSophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
||
S0398 |
AstemizoleAstemizole (R 43512) 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. |
||
S0188 |
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. |
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S5773 |
NS1643NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. |
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S4439 |
Almitrine mesylateAlmitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca2+-dependent K+ channel by decreasing its open probability with IC50 of 0.22 μM. |
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S0476 |
SCH-23390 hydrochlorideSCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) 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. |
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S2967 |
XE991 dihydrochlorideXE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively. |
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S6627 |
E-4031 dihydrochlorideE-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
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E0030New |
NS309NS309 is a potent and selective activator of human Ca2+ -activated K+ channels of SK and IK types with an EC50 of 150 nM for hSK3 channel, and displays no activity at BK channels. |
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S0050 |
ML277ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4. |
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S6559 |
ML-297ML-297 (VU 0456810, CID 56642816) 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. |
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S6553 |
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. |
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S0144 |
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. |
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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. |
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S0462 |
NS-1619NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
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S0467 |
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. |
||
E0034New |
CyPPACyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels. |
||
S0075 |
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. |
||
S6653 |
Nigericin (NSC 292567) sodium saltNigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
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. |
||
S4489 |
Tetraethylammonium chlorideTetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties. |
||
S4495 |
QuinineQuinine, an alkaloid derived from the bark of the cinchona tree, is an anti-malaria agent and a potassium channel inhibitor that inhibits mSlo3 (KCa 5.1) channel currents evoked by voltage pulses to +100 mV with IC50 of 169 μM. |
||
S4681 |
Quinidine hydrochloride monohydrateQuinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM. |
||
S9223 |
TalatisamineTalatisamine, a delphinine type alkaloid extracted from Aconitum talassicum, is a newly identified K+ channel blocker with hypotensive and antiarrhythmic activities. |
||
E0144New |
Vernakalant (RSD1235) HydrochlorideVernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period. |
||
E0015New |
IberiotoxinIberiotoxin (IbTX) is a toxin purified from the scorpion Buthus tamulus. Iberiotoxin is a potent blocker of the large conductance Ca(2+)-activated K+ channel with a Kd of ~1 nM. |
||
E0012New |
1-EBIO1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells. |
||
E0001New |
DCPIBDCPIB is a specific and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB potently inhibits several K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3. DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. DCPIB is also a novel selective blocker of I(Cl,swell), which blocks native I(Cl,swell) of calf bovine pulmonary artery endothelial (CPAE) cells with an IC(50) of 4.1 μM. |
||
S0524 |
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. |
||
S3242 |
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. |
||
S0741 |
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. |
||
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. |
||
S0087 |
JNJ 303JNJ 303 is a potent blocker of the voltage dependent IKs-channel encoded by KCNQ1/KCNE1 with IC50 of 64 nM. JNJ 303 induces QT-prolongations and causes unprovoked torsades de pointes (TdP). |
||
S6554 |
ML365ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
||
S2405 |
SophocarpineSophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
||
S0398 |
AstemizoleAstemizole (R 43512) 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. |
||
S0188 |
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. |
||
S5773 |
NS1643NS1643 is one of the small molecule HERG (Kv11.1) channel activators and has also been found to increase erg2 (Kv11.2) currents. |
||
S4439 |
Almitrine mesylateAlmitrine mesylate (Almitrine bismesylate, Almitrine dimethanesulfonate, Almitrine dimesylate), a pharmacologically unique respiratory stimulant, acts as an agonist of peripheral chemoreceptors located on the carotid bodies. Almitrine mesylate inhibits the activity of Ca2+-dependent K+ channel by decreasing its open probability with IC50 of 0.22 μM. |
||
S0476 |
SCH-23390 hydrochlorideSCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) 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. |
||
S2967 |
XE991 dihydrochlorideXE 991 (LS190926) dihydrochloride is a blocker of Kv7 (KCNQ) channels that potently inhibits KCNQ1 (Kv7.1), KCNQ2 (Kv7.2), KCNQ2 + KCNQ3 (Kv7.3) channel, and M-current with IC50 of 0.75 μM, 0.71 μM, 0.6 μM, and 0.98 μM, respectively. |
||
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 |
---|---|---|---|
E0030New |
NS309NS309 is a potent and selective activator of human Ca2+ -activated K+ channels of SK and IK types with an EC50 of 150 nM for hSK3 channel, and displays no activity at BK channels. |
||
S0050 |
ML277ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4. |
||
S6559 |
ML-297ML-297 (VU 0456810, CID 56642816) 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. |
||
S6553 |
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. |
||
S0144 |
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. |
||
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. |
||
S0462 |
NS-1619NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
||
S0467 |
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. |
Catalog No. | Information | Product Use Citations | Product Validations |
---|---|---|---|
E0034New |
CyPPACyPPA is a subtype-selective positive modulator of SK channels with EC50s of 5.6 μM and 14 μM for hSK3 and hSK2, repectively. CyPPA is inactive on both hSK1 and hIK channels. |
||
S0075 |
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 |
---|---|---|---|
S6653 |
Nigericin (NSC 292567) sodium saltNigericin (NSC 292567) sodium salt is an antibiotic derived from Streptomyces hygroscopicus that works by acting as an H+, K+, and Pb2+ ionophore.Nigericin can activate NLRP3 inflammasome to induce pro-inflammatory and immunostimulatory processes. |