Licensed by Pfizer Catalog No.S1716
Molecular Weight(MW): 494
Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
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|Description||Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.|
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. 
|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. |
-  Winquist RJ, et al. J Pharmacol Exp Ther,?989, 248(1), 149-156.
-  Nieland TJ, et al. J Lipid Res,?004, 45(7), 1256-1265.
-  Brady PA, et al. Eur J Pharmacol,?996, 308(3), 343-349.
|In vitro||DMSO||99 mg/mL (200.4 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+corn oil
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02864953||Not yet recruiting||Brain Edema|Stroke, Acute||Remedy Pharmaceuticals, Inc.||February 2017||Phase 3|
|NCT02919345||Not yet recruiting||Diabetes Mellitus, Type 2|Coronary Artery Disease|Carotid Artery Diseases||University of Campinas, Brazil|AstraZeneca||January 2017||Phase 4|
|NCT02460874||Not yet recruiting||Cerebral Edema|Brain Metastases||University of Maryland||December 2016||Phase 1|Phase 2|
|NCT02726490||Recruiting||Gestational Diabetes||Texas Tech University Health Sciences Center, El Paso||July 2016||--|
|NCT02830048||Recruiting||Diabetes Mellitus, Type 2||University of Oxford|Oxford University Hospitals NHS Trust||July 2016||Phase 2|
|NCT02375828||Completed||Neonatal Diabetes Secondary to Mutation in the Potassium Channel||Assistance Publique - Hôpitaux de Paris||March 2015||Phase 3|
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