CAS NO: | 10238-21-8 |
生物活性 | Glibenclamide (Glyburide) is an orally active ATP-sensitive K+channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibitsP-glycoprotein. Glibenclamide directly binds and blocks theSUR1subunits ofKATPand inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induceautophagy[5]. | ||||||||||||||||
IC50& Target | KATP[1] | ||||||||||||||||
体外研究 (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 (KATP) and consequently increases insulin secretion from the pancreatic β cells[2]. Glibenclamide interferes with mitochondrial bioenergy by permeating mitochondrial intima with Cl-and promoting mitochondrial net Cl-/K+cotransport[4]. Glibenclamide induced autophagy inhibits its insulin secretion-improving function in β cells[5]. | ||||||||||||||||
体内研究 (In Vivo) | Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level[2].
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Clinical Trial | |||||||||||||||||
分子量 | 494.00 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H28ClN3O5S | ||||||||||||||||
CAS 号 | 10238-21-8 | ||||||||||||||||
中文名称 | 格列本脲;优降糖;达安疗;达安宁;乙磺己脲;优格鲁康;氯磺环己脲;格列苯脲 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(506.07 mM;Need ultrasonic) H2O : 0.1 mg/mL(0.20 mM;Need ultrasonic and warming) 配制储备液
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以下溶剂前显示的百
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