Glyburide (Glibenclamide)

InformationGlyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.In vitroGlyburide (0.03 mM), a sulfonylurea which has been shown to block the ATP-modulated potassium channel in insulin-secreting cells, causes concentration-dependent shifts to the right (up to 100-fold) of the IC50 value for BRL 34915 and diazoxide, and at 1 μM, abolishes the relaxation response to minoxidil sulfate. Glyburide increases the apparent affinity of HDL binding to Scavenger receptor class B type I (SR-BI). Glyburide blocks SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC50 approximately 275-300 mM). Glyburide (6 mM) which reduces the opening of KATP channels, aggravates Ca2+ loading only when applied to dinitrophenol-pretreated myocytes but not when applied with dinitrophenol treatment. Glyburide (10-500 nM) produces a dose-dependent inhibition of the potassium channel openers (PCOs) relaxation time course. Glyburide also reverses existing Pinacidil relaxation regardless of the degree of pre-existing relaxation. Glyburideis is able to produce its blockade regardless of the state of K+ channel activation.In vivoGlyburide (GLY) dose-dependently increases urinary Na+ excretion with little change in urinary K+ excretion after i.p. administration (10-100 mg/kg) in saline-loaded conscious rats. Glyburide (25 mg/kg i.v.) increases Na+ excretion 350% during the first hour post-treatment without affecting K+ excretion, glomerular filtration rate, mean arterial pressure or heart rate.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specifications and Purity: 10mM in DMSO. Molecular Formula: C23H28ClN3O5S. Molecular Weight: 494.