Glibenclamide

格列本脲 (Glyburide) 是一种具有口服活性的 ATP 敏感性 K+ 通道 (KATP) 抑制剂，可用于糖尿病和肥胖症的研究。

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500mg

￥375.00

300.00

- +
1g

￥550.00

440.00

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Background

Glibenclamide(Glyburide) is a sulfonylurea compound that modulates insulin production. IC50 value:Target:Sulfonylureas bind to ATP-dependent K+ channels in beta cells of the pancreas, depolarizing them and stimulating the release of Ca2+, which in turn stimulates insulin production. Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim-activated K+ channels in smooth muscle. Binding of Gli to SUR produces the closure of KATP channels and the inhibition of their activity. Glibenclamide is widely used for treatment of type 2-diabetes and it has been signaled as antiproliferative in several tumor cell lines.

参考文献:
[1]. Núnez M, Medina V, Cricco G, et al. Glibenclamide inhibits cell growth by inducing G0/G1 arrest in the human breast cancer cell line MDA-MB-231. BMC Pharmacol Toxicol. 2013 Jan 11;14(1):6.
[2]. Soydan N, Bretzel RG, Fischer B, et al. Reduced capacity of heart rate regulation in response to mild hypoglycemia induced by glibenclamide and physical exercise in type 2 diabetes. Metabolism. 2013 Jan 11. pii: S0026-0495(12)00456-8.
[3]. Sokolovska J, Isajevs S, Sugoka O, et al. Comparison of the Effects of Glibenclamide on Metabolic Parameters, GLUT1 Expression, and Liver Injury in Rats With Severe and Mild Streptozotocin-Induced Diabetes Mellitus. Medicina (Kaunas). 2012;48(10):532-43.
[4]. Gangji AS, Cukierman T, Gerstein HC et al. A systematic review and meta-analysis of hypoglycemia and cardiovascular events: a comparison of glyburide with other secretagogues and with insulin. Diabetes Care. 2007 Feb;30(2):389-94.