product name Glyburide (Glibenclamide)
Description: Glyburide (also known as Glibenclamide) is a known 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.
494
Formula
C23H28ClN3O5S
CAS No.
10238-21-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 99 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Glyburide (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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 1989 Jan;248(1):149-56; J Pharmacol Exp Ther. 1993 May;265(2):933-7. |
