Glyburide (Glibenclamide)

For research use only.

Licensed by Pfizer Catalog No.S1716

1 publication

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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10mM (1mL in DMSO) USD 163 In stock
USD 122 In stock
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Selleck's Glyburide (Glibenclamide) has been cited by 1 publication

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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.
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 MmnOSpVv[3Srb36gZZN{[Xl? MVyxJIg> M1LIb3N1cW23bHH0bY9vKG:oIHnud5VtcW5ic3XjdoV1cW:wIHnuJJJifCCLTmOtNWUh[2WubIOgZYZ1\XJiMTDodkBjgSCjbIDoZWxKW0FiYYPzZZkhcW5icILld4Vv[2Vib3[gOUBuVSCpbIXjc5NmNCCHQ{WwQVAvODB|IN88US=> M1j4cFI1PDh2OUCw
CHO cells NEi2V|JHfW6ldHnvckBie3OjeR?= NVXuZmloUW6qaXLpeIlwdiCxZjDoeY1idiCVVWKxM2tqejZwMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{NCCLQ{WwQVAvODB2MzFOwG0> MVyxNVM2PjB7OR?=
HEK293 cells NH;admpHfW6ldHnvckBie3OjeR?= MnvWTY5pcWKrdHnvckBw\iCRQWTQNWIyKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{B2e2mwZzDld5Rz[WSrb3ytNVdj\XSjLXfseYN2em:waXTlJJN2[nO2cnH0[UwhUUN3ME2xMlQh|ryP MVGyNlU5Pzl6Nh?=

... 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]


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


CAS No. 10238-21-8
Storage powder
in solvent
Synonyms N/A
Smiles COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

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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 Active not recruiting 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 Not Applicable
NCT02830048 Completed Drug: Glibenclamide Diabetes Mellitus Type 2 University of Oxford|Oxford University Hospitals NHS Trust July 2016 Phase 2
NCT02375828 Completed Drug: Glibenclamide Neonatal Diabetes Secondary to Mutation in the Potassium Channel Assistance Publique - Hôpitaux de Paris March 20 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