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BMS-903452

Catalog No. T67791 CAS 1339944-47-6

BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 < 40 μM), did not activate PXR (EC50<50 μM), and was not toxic to liver (HEPG2) cell lines.

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BMS-903452, CAS 1339944-47-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 258.00
5 mg	In stock	$ 642.00
10 mg	In stock	$ 913.00
25 mg	In stock	$ 1,370.00
50 mg	In stock	$ 1,850.00
100 mg	In stock	$ 2,500.00
500 mg	In stock	$ 4,900.00
1 mL * 10 mM (in DMSO)	In stock	$ 753.00

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Purity: 100%

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Description	BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines.
Targets&IC50	GPR119:14nM(EC50)
In vivo	An oral glucose tolerance test (OGTT) to measure the acute efficacy of this agonist in C57/BL6 mice. Glucose excursion was 37%-40% lower in mice treated with BMS-903452 (0.1, 0.3, and 1 mg/kg) than in control mice. Treatment of SD rats with 0.3 mg/kg BMS-903452 stimulated GLP-1 production, and co-administration of BMS-903452 with a DPP-4 inhibitor synergistically augmented GLP-1 levels. [1] BMS-903452 (0.03 mg/kg/day) also reduced fasting plasma glucose levels with increased insulin levels in db/db mice. [1] BMS-903452 was safe and tolerable in normal healthy volunteers given a single dose ranging from 0.1 to 120mg, but did not alter plasma GLP-1 within the first 24 h of treatment.[2]

Molecular Weight	513.37
Formula	C21H19Cl2FN4O4S
CAS No.	1339944-47-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (19.48 mM)

References and Literature

1. Wacker DA, et al. Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119. J Med Chem. 2014;57(18):7499-7508. 2. Ritter K, et al. G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges. J Med Chem. 2016;59(8):3579-3592.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library GPCR Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max Clinical Compound Library Bioactive Compound Library

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Keywords

BMS-903452 1339944-47-6 Endocrinology/Hormones GPCR/G Protein GPR inhibitor inhibit

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