Repaglinide

Catalog No.S1426 Synonyms: AG-EE 623 ZW

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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In DMSO USD 90 In stock
USD 97 In stock
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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.
Targets
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]

Protocol

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
Formula

C27H36N2O4

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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03028103 Not yet recruiting Diffuse Large B Cell Lymphoma|Primary Mediastinal Lymphoma|Mantle Cell Lymphoma Epizyme, Inc. January 2017 Phase 1
NCT02836704 Recruiting Diabetes Mellitus, Type 2 Sanofi September 2016 Phase 4
NCT02694263 Recruiting Diabetes Mellitus, Type 2 University of Leicester|University Hospital Birmingham July 2016 Phase 4
NCT02305901 Completed Healthy Boehringer Ingelheim December 2014 Phase 1
NCT02128321 Completed Pharmacokinetics of Repaglinide|Pharmacokinetics of Caffeine|Healthy Subjects Astellas Pharma Global Development, Inc.|Basilea Pharmaceutica International Ltd|Astellas Pharma Inc January 2014 Phase 1
NCT01780051 Completed Diabetes Mellitus, Type 2 Dalim BioTech Co., Ltd. March 2013 Phase 1

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Potassium Channel Signaling Pathway Map

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