| Bioactivity | 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 inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and 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 induce autophagy[5]. | ||||||||||||
| Target | KATP | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level[2].Glibenclamide (50 μg/kg; p.o.) does not cause significant change, such as body weight or body composition[2]. Animal Model: | ||||||||||||
| Name | Glibenclamide | ||||||||||||
| CAS | 10238-21-8 | ||||||||||||
| Formula | C23H28ClN3O5S | ||||||||||||
| Molar Mass | 494.00 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Heo R, et al. The anti-diabetic drug trelagliptin induces vasodilation via activation of Kv channels and SERCA pumps. Life Sci. 2021;283:119868. [2]. Qiu Y, et al. Glyburide Regulates UCP1 Expression in Adipocytes Independent of KATP Channel Blockade. iScience. 2020;23(9):101446. [3]. Golstein PE, et al. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999;437(5):652-660. [4]. Fernandes MA, et al. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. J Biochem Mol Toxicol. 2004;18(3):162-169. [5]. Zhou J, et al. Glibenclamide-Induced Autophagy Inhibits Its Insulin Secretion-Improving Function in β Cells. Int J Endocrinol. 2019;2019:1265175. |
Glibenclamide
CAS: 10238-21-8 F: C23H28ClN3O5S W: 494.00
Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research
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