Glyburide (Glibenclamide)

Licensed by Pfizer Catalog No.S1716

Glyburide (Glibenclamide) Chemical Structure

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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In DMSO USD 130 In stock
USD 97 In stock
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Biological Activity

Description Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
Targets
Potassium channel [1]
In vitro

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. [1] 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). [2] 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. [3] 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. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
INS-1E cells M{DqfWZ2dmO2aX;uJIF{e2G7 NIfLcnYyKGh? MlmyV5RqdXWuYYTpc44hd2ZiaX7zeYxqdiC|ZXPy[ZRqd25iaX6gdoF1KEmQUz2xSUBk\WyuczDh[pRmeiBzIHjyJIJ6KGGucHjhUGlUSSCjc4PhfUBqdiCycnXz[Y5k\SCxZjC1JI1OKGeudXPvd4UtKEWFNUC9NE4xODNizszN MWeyOFQ5PDlyMB?=
CHO cells M1L0NGZ2dmO2aX;uJIF{e2G7 MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNWWjFxS3nyOk4zKGW6cILld5Nm\CCrbjDDTG8h[2WubIOsJGlEPTB;MD6wNFQ{KM7:TR?= NITORpoyOTN3NkC5PS=>
HEK293 cells M13pNWZ2dmO2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKE:DVGCxRlEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJJV{cW6pIHXzeJJi\GmxbD2xO4JmfGFvZ3z1Z5Vzd26rZHWgd5Vje3S{YYTlMEBKSzVyPUGuOEDPxE1? NFnielAzOjV6N{m4Oi=>

... Click to View More Cell Line Experimental Data

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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 99 mg/mL (200.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+corn oil
10mg/mL (suspension)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 494
Formula

C23H28ClN3O5S

CAS No. 10238-21-8
Storage powder
Synonyms N/A

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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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Potassium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID