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Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. - Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
- Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
- Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
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Potassium Channel inhibitor
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. -
potassium-competitive acid Blocker
TAK-438 is a novel potassium-competitive acid blocker. -
Kv1.3 blocker
PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
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NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
KATP channel antagonist
Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells. -
Potassium Channel Blocker
TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.- Samuel Drinkall, .et al. , Glia, 2022, Jul;70(7):1301-1316 PMID: 35353387
- Cheong Hoon Seo, .et al. , Transl Res, 2021, Apr 24 PMID: 33905948
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K+ channel blocker?€?
E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr). -
KCa2.1 channels activator
GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2). -
sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Ion channel blocker
Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.- Joe Z.Zhang, .et al. , Cell Stem Cell, 2019, 24, 1-10 PMID: 30880024
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Potassium channel blocker
Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β. -
K+ Channel inhibitor
K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur). -
Kir2 family channels inhibitor
ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5. -
Potassium channel blocker
Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk. - Citronellal or rhodinal or 3,7-dimethyloct-6-en-1-al is a monoterpenoid, the main component in the mixture of terpenoid chemical compounds that give citronella oil its distinctive lemon scent.
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potassium-competitive acid blocker
Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM. - Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
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Peripheral chemoreceptor agonist
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel. -
Kir7.1 potassium channels blocker
ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy. -
Kv3 voltage-gated potassium channel modulator
Kv3 modulator 1 is a Kv3 voltage-gated potassium channel modulator extracted from patent WO2018020263A1, Compound X. Kv3 modulator 1 can be used to treat inflammatory pain. -
potassium channel (non-GIRK1/X) activator
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel. -
KCNQ2/Q3 potassium channel activator
ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM. -
HERG activator
RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes. -
inhibitor of KCNJ1
KCNJ1 (Kir1.1, or renal outer medullary potassium channel) and KCNJ13 (Kir7.1) are inwardly rectifying two-transmembrane K+ channels. KCNJ1 has critical roles in kidney function, while KCNJ13 is important in the eye, kidney, and small intestine. VU590 is a small molecule inhibitor of KCNJ1 (IC50 = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 ?M. It has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 ?M. -
potassium currents blocker
Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.