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. |
-
Nat Commun, 2024, 15(1):1669
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
|
|
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. |
-
J Colloid Interface Sci, 2024, 664:338-348
-
Virus Res, 2024, 339:199258
-
Cell Mol Immunol, 2022, 19(8):925-943
|
|
S6653 |
Nigericin sodium salt
|
Nigericin 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. |
-
Biomed Pharmacother, 2024, 174:116548
-
Neural Regen Res, 2024, 19(10):2270-2280
-
EMBO J, 2023, e113118.
|
|
S1979 |
Amiodarone HCl
|
Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias. |
-
Cell Rep Methods, 2023, 3(4):100440
-
Cell Rep Methods, 2023, 3(4):100440
-
Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440
|
|
S2443 |
Tolbutamide (HLS 831)
|
Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes. |
-
Adv Healthc Mater, 2024, e2303785.
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1716 |
Glyburide (Glibenclamide)
|
Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes. |
-
Cell Chem Biol, 2023, S2451-9456(23)00335-5
-
BMC Vet Res, 2022, 18(1):145
-
Front Cell Infect Microbiol, 2021, 11:691445
|
|
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
|
|
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 Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. |
-
Pflugers Arch, 2023, 475(3):405-416
-
Cell Mol Immunol, 2022, 19(8):925-943
-
Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
|
|
S1971 |
Nicorandil
|
Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). |
-
J Cardiovasc Pharmacol Ther, 2022, 27:10742484221088655
-
BMC Cardiovasc Disord, 2021, 21(1):302
-
Sci Rep, 2017, 7(1):3156
|
|
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). |
-
Cancers (Basel), 2022, 14(19)4883
-
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
-
Cell Syst, 2019, 8(2):97-108
|
|
S2825 |
ML133 HCl
|
ML133 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. |
-
Cell Mol Immunol, 2022, 19(8):925-943
-
Nat Commun, 2022, 13(1):3544
-
Mol Pain, 2019, 15:1744806919838947
|
|
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. |
-
Acta Pharm Sin B, 2023, 13(1):142-156
-
Acta Pharm Sin B, 2023, 13(1):142-156
-
Biogerontology, 2016, 17(5-6):907-920
|
|
S4734 |
Retigabine 2HCl
|
Retigabine 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. |
-
J Biol Chem, 2021, S0021-9258(21)00985-6
-
Front Physiol, 2021, 12:790580
-
J Neurosci, 2020, 40(34):6522-6535
|
|
S2405 |
Sophocarpine
|
Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
-
J Med Virol, 2019, 91(8):1440-1447
-
Int J Biol Sci, 2019, 15(11):2497-2508
-
Front Pharmacol, 2019, 10:1219
|
|
S3151 |
Gliquidone
|
Gliquidone (Glurenorm,AR-DF 26) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM. |
-
Front Aging Neurosci, 2021, 13:754123
-
Front Cell Dev Biol, 2020, 8:269
-
Drug Test Anal, 2018, 10(3):609-617
|
|
S0476 |
SCH-23390 hydrochloride
|
SCH-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. |
-
Theranostics, 2023, 13(10):3149-3164
-
JCI Insight, 2023, 8(16)e170434
-
JCI Insight, 2023, 8(16)e170434
|
|
S2489 |
Nateglinide
|
Nateglinide (Starlix,A-4166,SDZ DJN 608) 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
|
|
S1715 |
Glipizide
|
Glipizide (CP-28720,K 4024) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. |
-
Cell Chem Biol, 2023, S2451-9456(23)00335-5
-
Front Pharmacol, 2022, 13:1046269
|
|
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. |
-
Br J Pharmacol, 2022, 10.1111/bph.15896
-
Free Radic Biol Med, 2017, 112:616-630
|
|
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.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
-
Toxicol Appl Pharmacol, 2022, 441:115988
-
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
|
|
S1344 |
Glimepiride
|
Glimepiride(HOE-490) 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
|
|
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
|
|
S1383 |
Minoxidil
|
Minoxidil (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. |
-
Oncotarget, 2016, 7(43):69703-69717
|
|
S2502 |
Quinine HCl Dihydrate
|
Quinine HCl Dihydrate is a white crystalline K+ channel blocker, used to treat malaria. |
-
J Pharmacol Toxicol Methods, 2017, 90:39-47
|
|
S2601 |
Gliclazide
|
Gliclazide(S1702, SE1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. |
-
IET Syst Biol, 2021, 10.1049/syb2.12034
|
|
S4681 |
Quinidine hydrochloride monohydrate
|
Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM. |
-
J Biomed Res, 2021, 35(5):395-407
|
|
S5257 |
Doxapram
|
Doxapram 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. |
-
Biomed Chromatogr, 2018, 32(10)
|
|
E0378 |
PAP-1
|
PAP-1 (5-(4-phenoxybutoxy)psoralen), a Kv1.3 antagonist with an EC50 of 2 nM, inhibits the proliferation of human T cells and suppresses delayed type hypersensitivity in rats.
|
-
Eur J Med Chem, 2023, 259:115561
-
Eur J Pharmacol, 2022, 933:175242
|
|
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. |
|
|
S6978 |
VU0071063
|
VU0071063 activates heterologously expressed Kir6.2/SUR1 channels with a EC50 of 7 μM, dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca2+ entry and insulin secretion. |
|
|
S4489 |
Tetraethylammonium chloride
|
Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties. |
|
|
S4495 |
Quinine
|
Quinine, 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. |
-
Cell Mol Immunol, 2022, 19(8):925-943
-
J Pharmacol Toxicol Methods, 2017, 90:39-47
|
|
S6284 |
Tetraethylammonium bromide
|
Tetraethylammonium bromide (TEAB, TEA 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. |
|
|
S0524 |
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. |
|
|
S3242 |
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 KATP current, influx of Ca2+ to the intracellular. |
|
|
S5371 |
Ajmaline
|
Ajmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. |
|
|
S0741 |
A2764 dihydrochloride
|
A2764 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. |
|
|
S6174 |
NS8593 Hydrochloride
|
NS8593 is a potent negative gating inhibitor of small conductance Ca2+
-activated K+ channels (SK1-3 or Kca2.1-2.3 channels). NS8593 is also a potent inhibitor of the TRPM7 channel with an IC50 of 1.6 µM. |
-
Int J Biol Macromol, 2024, 260(Pt 2):129454
|
|
E4828New |
Cloperastine fendizoate
|
Cloperastine fendizoate (Hustazol) is a sedative used to relieve cough and also has a peripheral action that desensitizes the afferent nerves in the tracheobronchial region. It inhibits the hERG K+ currents in a concentration-dependent manner, with an IC50 value of 0.027 μM. |
|
|
S0050 |
ML277
|
ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4. |
|
|
E4806New |
Quinine dihydrochloride
|
Quinine dihydrochloride is an antiparasitic used to treat malaria and is particularly important for managing malaria during the first trimester of pregnancy. It inhibits Slo3 (KCa 5.1) channel, which are a significant part of the mammalian KSper (sperm potassium conductance), by binding to hydrophobic side chains located at the intracellular region of the channel pore. |
|
|
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. |
|
|
S0311 |
SKA-31
|
SKA-31(Naphtho[1,2-d]thiazol-2-ylamine) is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. |
|
|
S4583 |
Butamben
|
Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain. |
|
|
E0012 |
1-EBIO
|
1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.
|
|
|
E0001 |
DCPIB
|
DCPIB 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. |
|
|
S0075 |
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. |
|
|
S0087 |
JNJ 303
|
JNJ 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). |
|
|
S6559 |
ML-297
|
ML-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 |
ML213
|
ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively. |
|
|
S0090 |
NS6180
|
NS-6180 is a highly selective inhibitor of KCa3.1 ion channel with IC50 value of 9 nM, which inhibits T cell activation and inflammation. |
|
|
E0501 |
Senicapoc (ICA-17043)
|
Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM. |
|
|
S6554 |
ML365
|
ML365 is a novel selective small molecule inhibitor of the TASK1 or potassium channel, subfamily K, member 9 (KCNK3). |
|
|
E0325 |
NS3623
|
NS3623 is an activator of human ether-a-go-go-related gene hERG1/KV11.1 potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels. |
|
|
S4186 |
Domiphen Bromide
|
Domiphen bromide (NSC-39415) is a quaternary ammonium antiseptic with actions as a cationic surfactant. |
|
|
E0105 |
ICA-27243
|
ICA-27243, a selective activator of the neuronal M current and KCNQ2/Q3 channels, induces a concentration-dependent increase in a 86Rb+ efflux from CHO cells expressing KCNQ2/Q3 channels with EC50 of 0.2 μM. |
|
|
S5028 |
4-Aminopyridine
|
4-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.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
|
|
S0144 |
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. |
|
|
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. |
|
|
S0398 |
Astemizole
|
Astemizole (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. |
|
|
E0030 |
NS309
|
NS309 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.
|
|
|
S0188 |
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. |
|
|
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. |
|
|
S4353 |
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. |
|
|
E1632New |
VU0463271
|
VU0463271 is a selective and potent antagonist of neuronal-specific potassium-chloride cotransporter 2 KCC2, with an IC50 of 61 nM. VU0463271 demonstrates over 100-fold selectivity compared to the closely related Na-K-2Cl cotransporter 1 (NKCC1). |
|
|
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. |
|
|
S4439 |
Almitrine mesylate
|
Almitrine 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. |
|
|
S0462 |
NS-1619
|
NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
|
|
S0467 |
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. |
|
|
E0034 |
CyPPA
|
CyPPA 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.
|
|
|
E0015New |
Iberiotoxin TFA
|
Iberiotoxin TFA(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.
|
|
|
S2967 |
XE991 dihydrochloride
|
XE 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. |
|
|
E0144 |
Vernakalant (RSD1235) Hydrochloride
|
Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
|
|
|
S6627 |
E-4031 dihydrochloride
|
E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
-
Front Pharmacol, 2024, 15:1370676
|
|
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. |
- Nat Commun, 2024, 15(1):1669
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
|
|
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. |
- J Colloid Interface Sci, 2024, 664:338-348
- Virus Res, 2024, 339:199258
- Cell Mol Immunol, 2022, 19(8):925-943
|
|
S1979 |
Amiodarone HCl
|
Amiodarone HCl is a sodium/potassium-ATPase inhibitor and an autophagy activator, used to treat various types of cardiac dysrhythmias. |
- Cell Rep Methods, 2023, 3(4):100440
- Cell Rep Methods, 2023, 3(4):100440
- Cell Reports Methods, 2023, 10.1016/j.crmeth.2023.100440
|
|
S2443 |
Tolbutamide (HLS 831)
|
Tolbutamide (HLS 831) is an inhibitor of potassium channel, used for type II diabetes. |
- Adv Healthc Mater, 2024, e2303785.
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S1716 |
Glyburide (Glibenclamide)
|
Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes. |
- Cell Chem Biol, 2023, S2451-9456(23)00335-5
- BMC Vet Res, 2022, 18(1):145
- Front Cell Infect Microbiol, 2021, 11:691445
|
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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
|
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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 Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. |
- Pflugers Arch, 2023, 475(3):405-416
- Cell Mol Immunol, 2022, 19(8):925-943
- Diabetes Res Clin Pract, 2022, S0168-8227(22)00588-5
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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). |
- Cancers (Basel), 2022, 14(19)4883
- Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
- Cell Syst, 2019, 8(2):97-108
|
|
S2825 |
ML133 HCl
|
ML133 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. |
- Cell Mol Immunol, 2022, 19(8):925-943
- Nat Commun, 2022, 13(1):3544
- Mol Pain, 2019, 15:1744806919838947
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S2405 |
Sophocarpine
|
Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects. |
- J Med Virol, 2019, 91(8):1440-1447
- Int J Biol Sci, 2019, 15(11):2497-2508
- Front Pharmacol, 2019, 10:1219
|
|
S0476 |
SCH-23390 hydrochloride
|
SCH-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. |
- Theranostics, 2023, 13(10):3149-3164
- JCI Insight, 2023, 8(16)e170434
- JCI Insight, 2023, 8(16)e170434
|
|
S2489 |
Nateglinide
|
Nateglinide (Starlix,A-4166,SDZ DJN 608) 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
|
|
S1715 |
Glipizide
|
Glipizide (CP-28720,K 4024) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes. |
- Cell Chem Biol, 2023, S2451-9456(23)00335-5
- Front Pharmacol, 2022, 13:1046269
|
|
S1344 |
Glimepiride
|
Glimepiride(HOE-490) 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
|
|
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. |
- J Pharmacol Toxicol Methods, 2017, 90:39-47
|
|
S2601 |
Gliclazide
|
Gliclazide(S1702, SE1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. |
- IET Syst Biol, 2021, 10.1049/syb2.12034
|
|
S4681 |
Quinidine hydrochloride monohydrate
|
Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM. |
- J Biomed Res, 2021, 35(5):395-407
|
|
S5257 |
Doxapram
|
Doxapram 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. |
- Biomed Chromatogr, 2018, 32(10)
|
|
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. |
|
|
S4489 |
Tetraethylammonium chloride
|
Tetraethylammonium (TEA) chloride is a nonspecific potassium channel blocker with antitumor properties. |
|
|
S4495 |
Quinine
|
Quinine, 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. |
- Cell Mol Immunol, 2022, 19(8):925-943
- J Pharmacol Toxicol Methods, 2017, 90:39-47
|
|
S6284 |
Tetraethylammonium bromide
|
Tetraethylammonium bromide (TEAB, TEA 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. |
|
|
S0524 |
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. |
|
|
S3242 |
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 KATP current, influx of Ca2+ to the intracellular. |
|
|
S5371 |
Ajmaline
|
Ajmaline (Cardiorythmine, Tachmalin), found in the root of Rauwolfia serpentina, is a class Ia antiarrhythmic agent. |
|
|
S0741 |
A2764 dihydrochloride
|
A2764 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. |
|
|
S6174 |
NS8593 Hydrochloride
|
NS8593 is a potent negative gating inhibitor of small conductance Ca2+
-activated K+ channels (SK1-3 or Kca2.1-2.3 channels). NS8593 is also a potent inhibitor of the TRPM7 channel with an IC50 of 1.6 µM. |
- Int J Biol Macromol, 2024, 260(Pt 2):129454
|
|
E4828New |
Cloperastine fendizoate
|
Cloperastine fendizoate (Hustazol) is a sedative used to relieve cough and also has a peripheral action that desensitizes the afferent nerves in the tracheobronchial region. It inhibits the hERG K+ currents in a concentration-dependent manner, with an IC50 value of 0.027 μM. |
|
|
E4806New |
Quinine dihydrochloride
|
Quinine dihydrochloride is an antiparasitic used to treat malaria and is particularly important for managing malaria during the first trimester of pregnancy. It inhibits Slo3 (KCa 5.1) channel, which are a significant part of the mammalian KSper (sperm potassium conductance), by binding to hydrophobic side chains located at the intracellular region of the channel pore. |
|
|
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 (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain. |
|
|
E0012 |
1-EBIO
|
1-EBIO (1-Ethylbenzimidazolinone, 1-Ethyl-2-benzimidazolinone)is an activator of Ca2+-sensitive K+ channels with an EC50 of 490 µM in T84 cells.
|
|
|
E0001 |
DCPIB
|
DCPIB 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. |
|
|
S0087 |
JNJ 303
|
JNJ 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). |
|
|
S0090 |
NS6180
|
NS-6180 is a highly selective inhibitor of KCa3.1 ion channel with IC50 value of 9 nM, which inhibits T cell activation and inflammation. |
|
|
E0501 |
Senicapoc (ICA-17043)
|
Senicapoc (ICA-17043) is a Gardos channel(Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM and produces dose-dependent increases in hemoglobin and decreases in markers of hemolysis. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM. |
|
|
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. |
|
|
S5028 |
4-Aminopyridine
|
4-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.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
|
|
S0398 |
Astemizole
|
Astemizole (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 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. |
|
|
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. |
|
|
S4353 |
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. |
|
|
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. |
|
|
S4439 |
Almitrine mesylate
|
Almitrine 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. |
|
|
E0015New |
Iberiotoxin TFA
|
Iberiotoxin TFA(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.
|
|
|
S2967 |
XE991 dihydrochloride
|
XE 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. |
|
|
E0144 |
Vernakalant (RSD1235) Hydrochloride
|
Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
|
|
|
S6627 |
E-4031 dihydrochloride
|
E-4031 is an experimental class III antiarrhythmic drug that blocks potassium channels of the hERG-type. |
- Front Pharmacol, 2024, 15:1370676
|
|
S1971 |
Nicorandil
|
Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). |
- J Cardiovasc Pharmacol Ther, 2022, 27:10742484221088655
- BMC Cardiovasc Disord, 2021, 21(1):302
- Sci Rep, 2017, 7(1):3156
|
|
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. |
- Acta Pharm Sin B, 2023, 13(1):142-156
- Acta Pharm Sin B, 2023, 13(1):142-156
- Biogerontology, 2016, 17(5-6):907-920
|
|
S4734 |
Retigabine 2HCl
|
Retigabine 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. |
- J Biol Chem, 2021, S0021-9258(21)00985-6
- Front Physiol, 2021, 12:790580
- J Neurosci, 2020, 40(34):6522-6535
|
|
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. |
- Br J Pharmacol, 2022, 10.1111/bph.15896
- Free Radic Biol Med, 2017, 112:616-630
|
|
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.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing. |
- Toxicol Appl Pharmacol, 2022, 441:115988
- Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.04.011
|
|
S1383 |
Minoxidil
|
Minoxidil (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. |
- Oncotarget, 2016, 7(43):69703-69717
|
|
S6978 |
VU0071063
|
VU0071063 activates heterologously expressed Kir6.2/SUR1 channels with a EC50 of 7 μM, dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca2+ entry and insulin secretion. |
|
|
S0050 |
ML277
|
ML277 (CID-53347902) is a potent activator of KCNQ1 channels with an EC50 of 260 nM and shows >100-fold selectivity over KCNQ2 and KCNQ4. |
|
|
S0311 |
SKA-31
|
SKA-31(Naphtho[1,2-d]thiazol-2-ylamine) is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. |
|
|
S6559 |
ML-297
|
ML-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 |
ML213
|
ML213 (CID-3111211) is a selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) potassium channel opener with EC50 of 230 nM and 510 nM, respectively. |
|
|
E0325 |
NS3623
|
NS3623 is an activator of human ether-a-go-go-related gene hERG1/KV11.1 potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels. |
|
|
S0144 |
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. |
|
|
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. |
|
|
E0030 |
NS309
|
NS309 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.
|
|
|
S0462 |
NS-1619
|
NS-1619 is a selective activator of large conductance Ca2+-activated K+-channels. |
|
|
S0467 |
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. |
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