For research use only.

Catalog No.S1426 Synonyms: AG-EE 623 ZW

1 publication

Repaglinide Chemical Structure

Molecular Weight(MW): 452.59

Repaglinide 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.

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10mM (1mL in DMSO) USD 90 In stock
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Selleck's Repaglinide has been cited by 1 publication

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Biological Activity

Description Repaglinide 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.
Potassium channel [1]
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 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]


Solubility (25°C)

In vitro DMSO 91 mg/mL (201.06 mM)
Ethanol 91 mg/mL (201.06 mM)
Water 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 452.59


CAS No. 135062-02-1
Storage powder
in solvent
Synonyms AG-EE 623 ZW

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02128321 Completed Drug: Isavuconazole|Drug: Repaglinide|Drug: Caffeine Pharmacokinetics of Repaglinide|Pharmacokinetics of Caffeine|Healthy Subjects Astellas Pharma Global Development Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc January 2014 Phase 1
NCT01797198 Completed Drug: ASP3652|Drug: Gemfibrozil|Drug: Repaglinide Drug-Drug Interaction (DDI)|Healthy Subjects Astellas Pharma Europe B.V.|Astellas Pharma Inc April 2012 Phase 1

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Potassium Channel Signaling Pathway Map

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