For research use only.
Licensed by Pfizer Catalog No.S1716
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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|Description||Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.|
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.  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).  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.  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. 
|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. |
-  Winquist RJ, et al. J Pharmacol Exp Ther,?989, 248(1), 149-156.
-  Nieland TJ, et al. J Lipid Res,?004, 45(7), 1256-1265.
-  Brady PA, et al. Eur J Pharmacol,?996, 308(3), 343-349.
|In vitro||DMSO||99 mg/mL (200.4 mM)|
|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.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
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.
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