RGNCY-0005 (BMS903452, GPR119 agonist)

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BMS-903452 is a representative of new class of pyridone containing GPR119 agonist (hEC50 14nM) and is an anti-diabetic clinical candidate. This potent and selective compound was efficacious in both acute and chronic in vivo rodent models of diabetes. Dosing of BMS-903452 healthy humans in a single ascending dose study showed a dose dependent increase in exposure and a trend toward increased total GLP-1 plasma levels.

SMILES: CS(C1=CC=C(N2C=C(Cl)C(OC3CCN(C4=NC=C(Cl)C=N4)CC3)=CC2=O)C(F)=C1)(=O)=O

Systematic Name: 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one

Molecular Weight: 513.37

Formula: C21H19Cl2FN4O4S

Reference: Wacker, Dean A., et al. "Discovery of 5-Chloro-4-((1-(5-chloropyrimidin-2-yl) piperidin-4-yl) oxy)-1-(2-fluoro-4-(methylsulfonyl) phenyl) pyridin-2 (1 H)-one (BMS-903452), an Antidiabetic Clinical Candidate Targeting GPR119." Journal of Medicinal Chemistry 57.18 (2014): 7499 - 7508.

PMID: 25208139

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Tags: GPR119, Diabetes, RGNCY-0005, BMS903452