Other
CN
EU
USA
Description: Glyburide (also known as Glibenclamide) is a known and selective blocker of vascular ATP-sensitive K+ channels (KATP). Glyburide is an antidiabetic sulfonylurea derivative used in the treatment of type 2 diabetes. Its actions are similar to those of chlorpropamide that can potentially be used to decrease cerebral edema.
References: J Pharmacol Exp Ther. 1989 Jan;248(1):149-56; J Pharmacol Exp Ther. 1993 May;265(2):933-7.
Chemical Name: 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
InChi Key: ZNNLBTZKUZBEKO-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
SMILES Code: COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
HB-420; HB419; HB420; Glyburide; Glibenclamide; Glybenclamide; Micronase; Diabeta; Maninil; Micronase; Neogluconin
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Glyburide (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.
J Pharmacol Exp Ther. 1989 Jan;248(1):149-56; J Pharmacol Exp Ther. 1993 May;265(2):933-7.
Purity ≥98%
COA
MSDS