kir6.2/sur1

Mitiglinide calcium hydrate (S-21403 calcium hydrate) is a drug for the treatment of type 2 diabetes. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs and is currently co-marketed in Japan by Kissei and Takeda.

VU0071063 is a Kir6.2 SUR1 activator.

Mitiglinide Calcium (KAD-1229) is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.

Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.

ML418 is a potent, selective, and CNS-penetrating Kir7.1 potassium channel blocker (IC50 = 310 nM) that also effectively inhibits Kir6.2 SUR1.

Tifenazoxide is an effective and SUR1 Kir6.2 selective KATP channels opener. Tifenazoxide has an anti-diabetic effect, can inhibit glucose-stimulated insulin release in vitro and in vivo.

VU041 is an inhibitor of Anopheles gambiae and Aedes aegypti inward rectifier potassium 1 channels (IC50: 2.5 μM and 1.7 μM, respectively). VU041 inhibits appreciably is mammalian Kir2.1 (IC50: 12.7 μM) and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2 SUR1, and Kir7.1.

Mitiglinide (KAD-1229) is an insulinotropic agent that is an ATP-sensitive K + (K ATP ) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K ATP channel). Mitiglinide is able to be used for the research of type 2 diabetes [1] [2].

rac-trans-4-hydroxy Glyburide, an active metabolite of the SUR1 Kir6.2 sulfonylurea inhibitor glyburide, is formed by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. It inhibits glyburide binding to rat brain synaptosomes at high and low affinity sites of SUR1 Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.

Cibenzoline is an antiarrhythmic agent that inhibits the KATP channel by directly affecting the pore-forming Kir6.2 subunit rather than the SUR1 subunit. Cibenzoline shows little anticholinergic activity. Cibenzoline markedly reduces LVPG which has a close relationship with myocardial contractility decreasing. Cibenzoline has the potential for hypertrophic obstructive cardiomyopathy research[1][2].