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Glyburide (Glibenclamide)

Name: Glyburide (Glibenclamide)
Brand: Selleck Chemicals
SKU: S1716
Rating: 5 (7 reviews)

Synonyms: Glibenclamide

Catalog No.S1716 Purity: 99.93%

Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.

Glyburide (Glibenclamide) Chemical Structure

CAS: 10238-21-8

Selleck's Glyburide (Glibenclamide) has been cited by 7 publications

Purity & Quality Control

Batch: Purity: 99.93%

99.93

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Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
INS-1E cells	Function assay	1 h	Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose, EC50=0.003 μM	24484900
CHO cells	Function assay		Inhibition of human SUR1/Kir6.2 expressed in CHO cells, IC50=0.0043 μM	11356099
HEK293 cells	Function assay		Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=1.4 μM	22587986
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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
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]

In Vivo
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05426681	Recruiting	Acute Spinal Cord Injury	University of Kentucky	July 7 2022	Phase 1
NCT03832595	Completed	Chronic Kidney Diseases	University of Pittsburgh\|Vanderbilt University Medical Center\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	May 1 2019	Not Applicable

References

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Chemical lnformation & Solubility

Molecular Weight	494	Formula	C₂₃H₂₈ClN₃O₅S
CAS No.	10238-21-8	SDF	Download Glyburide (Glibenclamide) SDF
Smiles	COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 99 mg/mL ( (200.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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