Catalog No.S1426 Synonyms: AG-EE 623 ZW
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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|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.|
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.  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.  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. 
|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. |
|In vitro||DMSO||91 mg/mL (201.06 mM)|
|Ethanol||91 mg/mL (201.06 mM)|
* 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.
|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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