MCE products for research use only. We do not sell to patients.

Glibenclamide

MCE China：Glibenclamide

Brand：MedChemExpress (MCE)

Cat. No.HY-15206

CAS：10238-21-8

Synonyms：Glyburide

Purity：99.94%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.

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].

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].

IC50 & Target：KATP[1] Cellular Effect Cell Line Type Value Description References

Hot selling product：4-Chloro-7H-pyrrolo[2,3-d]pyrimidine  | SPB  | Tamibarotene  | CITCO  | Relugolix  | Cefoperazone  | LCMV gp33-41  | H-Phe(4-Ac)-OH  | 3-Nitropropanoic acid  | Demeclocycline

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[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.  [Content Brief]

[2]. Qiu Y, et al. Glyburide Regulates UCP1 Expression in Adipocytes Independent of KATP Channel Blockade. iScience. 2020;23(9):101446.  [Content Brief]

[3]. Golstein PE, et al. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999;437(5):652-660.  [Content Brief]

[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.  [Content Brief]

[5]. Zhou J, et al. Glibenclamide-Induced Autophagy Inhibits Its Insulin Secretion-Improving Function in β Cells. Int J Endocrinol. 2019;2019:1265175.  [Content Brief]