Glyburide (Glibenclamide)

Licensed by Pfizer Catalog No.S1716

For research use only.

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

Selleck's Glyburide (Glibenclamide) has been cited by 5 Publications

Purity & Quality Control

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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 MlXVSpVv[3Srb36gZZN{[Xl? M2rIZlEhcA>? M2W3eHN1cW23bHH0bY9vKG:oIHnud5VtcW5ic3XjdoV1cW:wIHnuJJJifCCLTmOtNWUh[2WubIOgZYZ1\XJiMTDodkBjgSCjbIDoZWxKW0FiYYPzZZkhcW5icILld4Vv[2Vib3[gOUBuVSCpbIXjc5NmNCCHQ{WwQVAvODB|IN88US=> NYn0dpdYOjR2OES5NFA>
CHO cells M{C5WmZ2dmO2aX;uJIF{e2G7 NFnEU|JKdmirYnn0bY9vKG:oIHj1cYFvKFOXUkGvT4lzPi5{IHX4dJJme3OnZDDpckBEUE9iY3XscJMtKEmFNUC9NE4xODR|IN88US=> NYPkeW46OTF|NU[wPVk>
HEK293 cells NEXYcXJHfW6ldHnvckBie3OjeR?= NFHGTVZKdmirYnn0bY9vKG:oIF;BWHAySjFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KHW|aX7nJIV{fHKjZHnvcE0yP2KndHGt[4x2[3W{b37p[IUhe3Wkc4TyZZRmNCCLQ{WwQVEvPCEQvF2= M2jnWlIzPTh5OUi2
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 (from reference)

Solubility (25°C)

In vitro

DMSO 99 mg/mL
(200.4 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.

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 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03832595 Enrolling by invitation Other: Intervention Arm|Other: Usual Care 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
NCT03791580 Unknown status Behavioral: Commitment nudge|Behavioral: Justification nudge Fall|Congestive Heart Failure|Chronic Kidney Failure|Adverse Drug Event RAND|Northwestern University|University of California Los Angeles|University of Southern California|University of Pittsburgh|National Institute on Aging (NIA) February 11 2019 Not Applicable
NCT02726490 Terminated Drug: Glyburide|Drug: Glucovance Gestational Diabetes Texas Tech University Health Sciences Center El Paso July 2016 Early Phase 1
NCT02830048 Completed Drug: Glibenclamide Diabetes Mellitus Type 2 University of Oxford|Oxford University Hospitals NHS Trust July 2016 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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