Glimepiride

Catalog No.S1344

Glimepiride Chemical Structure

Molecular Weight(MW): 490.62

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.

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  • (E) ELISA analysis for C-peptide levels in the presence of vehicle, diazoxide and glimepiride. (F) The fold change of C-peptide content after diazoxide and glimepiride stimulation. Diazoxide and glimepiride decreased and increased C-peptide secretion in wild-type and heterozygous mutated cells, respectively. Neither diazoxide nor glimepiride had an effect on homozygous mutated cells.

    Sci Rep., 2017, 7: 3156. Glimepiride purchased from Selleck.

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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

Solubility (25°C)

In vitro DMSO 11 mg/mL (22.42 mM)
Water Insoluble
Ethanol Insoluble

* 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 490.62
Formula

C24H34N4O5S

CAS No. 93479-97-1
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03009513 Not yet recruiting Diabetes Mellitus Handok Pharmaceuticals Co., Ltd. January 2017 Phase 1
NCT02985242 Recruiting Diabetes Mellitus, Type II Hannover Medical School December 2016 Phase 4
NCT02954822 Not yet recruiting Type2 Diabetes Dong-A ST Co., Ltd. November 2016 Phase 1
NCT02956044 Recruiting Type2 Diabetes Mellitus Theracos November 2016 Phase 1
NCT02964572 Not yet recruiting Type2 Diabetes Mellitus Yonsei University November 2016 --
NCT02919059 Not yet recruiting Diabetes Mellitus, Type 2 IInstituto Gallego de Medicina Vascular October 2016 Phase 4

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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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Potassium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID