Glimepiride

Catalog No.S1344

For research use only.

Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.

Glimepiride Chemical Structure

CAS No. 93479-97-1

Selleck's Glimepiride has been cited by 1 Publication

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Biological Activity

Description Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
Targets
SUR1 [1] SUR2A [1] SUR2B [1]
3 nM 5.4 nM 7.3 nM
In vitro

Glimepiride inhibits Kir6.2/SUR currents by interaction with two sites: a low-affinity site on Kir6.2 (IC(50)= approximately 400 mM) and a high-affinity site on SUR (IC(50)=3.0 nM for SUR1, 5.4 nM for SUR2A and 7.3 nM for SUR2B). [1] Glimepiride exhibits a higher potency compared to Glibenclamide with respect to stimulation of glucose transport, glucose transporter isoform 4 (GLUT4) translocation and lipid and glycogen synthesis in normal and insulin-resistant adipocytes and in muscle cells, as well as of the potential underlying signalling processes examined at the molecular level. Glimepiride associates in a time- and concentration dependent non-saturable manner with detergent-insoluble complexes of the plasma membrane which may correspond to caveolae. [2] Glimepiride blocks pinacidil-activated whole-cell K(ATP) currents of cardiac myocytes with an IC(50) of 6.8 nM, comparable to the potency of Glibenclamide in these cells. Glimepiride blocks K(ATP) channels formed by co-expression of Kir6.2/SUR2A subunits in HEK 293 cells in outside-out excised patches with a similar IC(50) of 6.2 nM. [3]

In vivo Glimepiride prevents the NA-STZ induced increased frequency of micronucleus (MN) in polychromatic and normochromatic erythrocytes. Glimepiride also decreases the sperm shape abnormality and enhances the sperm count besides improving the antioxidant status in the diabetic rats. Glimepiride inhibits the NA-STZ mediated changes in the MN frequency and sperm abnormality and enhanced the antioxidant defense. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 490.62
Formula

C24H34N4O5S

CAS No. 93479-97-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C

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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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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT02973477 Completed Drug: Dapagliflozin|Drug: Glimepiride Type2 Diabetes|Cardiovascular Diseases University of Michigan|AstraZeneca January 12 2017 Phase 4
NCT02919059 Unknown status Drug: Dapagliflozin 10 mg|Drug: Glimepiride 4 mg Diabetes Mellitus Type 2 IInstituto Gallego de Medicina Vascular December 13 2016 Phase 4
NCT02964572 Completed Drug: Glimepiride|Drug: Empagliflozin Type2 Diabetes Mellitus Yonsei University November 2016 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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