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

Repaglinide

Synonyms: AG-EE 623 ZW

Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.

Repaglinide Chemical Structure

Repaglinide Chemical Structure

CAS No. 135062-02-1

Purity & Quality Control

Repaglinide Related Products

Signaling Pathway

Potassium Channel Signaling Pathways

Potassium Channel Signaling Pathway

Biological Activity

Description Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.
Targets
Potassium channel [1]
In vitro
In vitro Repaglinide is found to bind with low affinity (K(D)=59 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 is co-expressed with Kir6.2. Repaglinide binds with low affinity (K(D)=51 nM) to SUR1 co-expressed with Kir6.2DeltaN14. [1] Repaglinide lowers the plasma glucose concentration in the control rat, whilst failing to affect significantly the plasma insulin concentration or insulin/glucose ratio. Repaglinide administration affects neither plasma glucose nor insulin concentration, restores a normal value for the otherwise abnormally high basal insulin output, increases the 16.7 mM/2.8 mM ratio for insulin release, and again augmented protein biosynthesis at both low and high hexose concentrations in Goto-Kakizaki (GK) rats. [2] Repaglinide is found to bind to NCS proteins, but not to CaM or S100 proteins, in a Ca2+-dependent manner. Repaglinide antagonizes the inhibitory action of recoverin in a rhodopsin kinase assay with IC50 values of 400 mM. Repaglinide tightly binds to the visinin-like domain of CCaMK and PpCaMK in a Ca2+-dependent manner and antagonizes the regulatory function of the domain with IC50 values of 55 and 4 mM for CCaMK and PpCaMK respectively. [3]
In Vivo
In vivo Repaglinide provokes a greater and more rapid increase in plasma insulin concentration and an earlier fall in glycemia than those observed after administration of the hypoglycemic sulfonylureas in both fed and starved normal rats. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06290050 Recruiting
Healthy Volunteers
Takeda
 March 29 2024 Phase 1

Chemical Information & Solubility

Molecular Weight 452.59 Formula

C27H36N2O4
CAS No. 135062-02-1 SDF Download Repaglinide SDF
Smiles CCOC1=C(C=CC(=C1)CC(=O)NC(CC(C)C)C2=CC=CC=C2N3CCCCC3)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (201.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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In vivo
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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.

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