For research use only. Not for therapeutic Use.
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells[1][2][3].
Treatment with BMS-309403 significantly decreased MCP-1 production from THP-1 macrophages in a dose- and time-dependent manner[1].
BMS-309403 sodium (15 mg/kg; chronic treatment; daily for 6 weeks) improves endothelial function, phosphorylated and total eNOS and reduced plasma triglyceride levels but did not affect endothelium-independent relaxations[3].
| Catalog Number | I045689 |
| CAS Number | 2802523-05-1 |
| Synonyms | sodium;2-[3-[2-(5-ethyl-3,4-diphenylpyrazol-1-yl)phenyl]phenoxy]acetate |
| Molecular Formula | C31H25N2NaO3 |
| Purity | ≥95% |
| InChI | InChI=1S/C31H26N2O3.Na/c1-2-27-30(22-12-5-3-6-13-22)31(23-14-7-4-8-15-23)32-33(27)28-19-10-9-18-26(28)24-16-11-17-25(20-24)36-21-29(34)35;/h3-20H,2,21H2,1H3,(H,34,35);/q;+1/p-1 |
| InChIKey | NZLJLBNAOJOVBZ-UHFFFAOYSA-M |
| SMILES | CCC1=C(C(=NN1C2=CC=CC=C2C3=CC(=CC=C3)OCC(=O)[O-])C4=CC=CC=C4)C5=CC=CC=C5.[Na+] |
| Reference | [1]. Sulsky R, et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett. 2007;17(12):3511-3515. [2]. Lin W, et al. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570. [3]. Lee MY, et al. Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells. Br J Pharmacol. 2011;162(7):1564-1576. |
