sur1

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

Glimepiride (HOE-490) is a long-acting, third-generation sulfonylurea with hypoglycemic activity.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)

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

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.

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.

VU0071063 is a Kir6.2/SUR1 activator.

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].

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.

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].

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.

Gliquidone-d6 is a deuterated compound of Gliquidone. Gliquidone has a CAS number of 33342-05-1. Gliquidone is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

Gliquidone sodium is a hypoglycemic sulfonylurea which may protect the liver from injury from diabetes.