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Glibenclamide

CAS No. : 10238-21-8

MCE 国际站：Glibenclamide

产品活性：Glibenclamide (Glyburide) 是一种具有口服活性的 ATP 敏感的 K⁺ 通道 (K_ATP) 抑制剂，可用于糖尿病和肥胖的研究。Glibenclamide 抑制 P-glycoprotein。Glibenclamide 直接结合并阻断K_ATP 的 SUR1 亚基并抑制囊性纤维化跨膜传导调节蛋白 (CFTR)。Glibenclamid 通过诱导膜离子通透性干扰线粒体生物能。Glibenclamid 可诱导自噬。

研究领域：Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease  |  Autophagy

作用靶点：Potassium Channel  |  Mitochondrial Metabolism  |  Autophagy  |  CFTR  |  P-glycoprotein

In Vitro: Glibenclamide (Brown adipocytes; 10 μΜ; 1 day) has no effect on adipocyte differentiation. Glibenclamide (Ucp1-2A-GFP brown adipocyte) significantly increases UCP1 expression. Glibenclamide directly binds and blocks the SUR1 subunits of ATP-dependent potassium channels (K_ATP) and consequently increases insulin secretion from the pancreatic β cells. Glibenclamide interferes with mitochondrial bioenergy by permeating mitochondrial intima with Cl^- and promoting mitochondrial net Cl^-/K⁺ cotransport. Glibenclamide induced autophagy inhibits its insulin secretion-improving function in β cells.

In Vivo: Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level.
Glibenclamide (50 μg/kg; p.o.) does not cause significant change, such as body weight or body composition.

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