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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 No. 10238-21-8

Purity & Quality Control

Batch: Purity: 99.93%

99.93

Glyburide (Glibenclamide) Related Products

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Signaling Pathway

Potassium Channel Signaling Pathway

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
Click to View More Cell Line Experimental Data

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 2024-05-22)
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 Information & 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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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