WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522370
Description: BMS-903452 is a potent and selective GRP119 agonist. BMS-903452 is efficacious in both acute and chronic in vivo rodent models of diabetes. Dosing of BMS-903452 in a single ascending dose study in normal healthy humans showed a dose dependent increase in exposure and a trend toward increased total GLP-1 plasma levels. G-protein-coupled receptor 119 (GPR119) is expressed predominantly in pancreatic β-cells and in enteroendocrine cells in the gastrointestinal tract. GPR119 agonists have been shown to stimulate glucose-dependent insulin release by direct action in the pancreas and to promote secretion of the incretin GLP-1 by action in the gastrointestinal tract. This dual mechanism of action has generated significant interest in the discovery of small molecule GPR119 agonists as a potential new treatment for type 2 diabetes.
MedKoo Cat#: 522370
Chemical Formula: C21H19Cl2FN4O4S
Exact Mass: 512.04881
Molecular Weight: 513.37
Elemental Analysis: C, 49.13; H, 3.73; Cl, 13.81; F, 3.70; N, 10.91; O, 12.47; S, 6.25
Synonym: BMS-903452; BMS 903452; BMS903452.
IUPAC/Chemical Name: 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one
InChi Key: OGIAVRWXUPYGGC-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H19Cl2FN4O4S/c1-33(30,31)15-2-3-18(17(24)8-15)28-12-16(23)19(9-20(28)29)32-14-4-6-27(7-5-14)21-25-10-13(22)11-26-21/h2-3,8-12,14H,4-7H2,1H3
SMILES Code: O=C1C=C(OC2CCN(C3=NC=C(Cl)C=N3)CC2)C(Cl)=CN1C4=CC=C(S(=O)(C)=O)C=C4F
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 513.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Wacker DA, Wang Y, Broekema M, Rossi K, O'Connor S, Hong Z, Wu G, Malmstrom SE, Hung CP, LaMarre L, Chimalakonda A, Zhang L, Xin L, Cai H, Chu C, Boehm S, Zalaznick J, Ponticiello R, Sereda L, Han SP, Zebo R, Zinker B, Luk CE, Wong R, Everlof G, Li YX, Wu CK, Lee M, Griffen S, Miller KJ, Krupinski J, Robl JA. 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 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v. Epub 2014 Sep 10. PubMed PMID: 25208139.