Home Transmembrane Transporters Potassium Channel inhibitor Glimepiride For research use only.

Glimepiride

Synonyms: HOE-490

Glimepiride(HOE-490) 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

Glimepiride Chemical Structure

CAS No. 93479-97-1

Purity & Quality Control

Glimepiride Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

Biological Activity

Description Glimepiride(HOE-490) 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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03791580 Unknown status
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
Type2 Diabetes|Cardiovascular Diseases
University of Michigan|AstraZeneca
 January 12 2017 Phase 4
NCT02919059 Unknown status
Diabetes Mellitus Type 2
IInstituto Gallego de Medicina Vascular
 December 13 2016 Phase 4
NCT02964572 Completed
Type2 Diabetes Mellitus
Yonsei University
 November 2016 Not Applicable

Chemical Information & Solubility

Molecular Weight 490.62 Formula

C24H34N4O5S
CAS No. 93479-97-1 SDF Download Glimepiride SDF
Smiles CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 11 mg/mL ( (22.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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