| Identification | Back Directory | [Name]
Acetic acid, 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-, sodium salt (1:1) | [CAS]
2802523-05-1 | [Synonyms]
Acetic acid, 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-, sodium salt (1:1)
Acetic acid, 2-[[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)[1,1'-biphenyl]-3-yl]oxy]-, sodium salt (1:1) | [Molecular Formula]
C31H27N2NaO3 | [MOL File]
2802523-05-1.mol | [Molecular Weight]
498.56 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | Animal Model: | C57BL/6J mice (ApoE?/? mice)[3] | | Dosage: | 15 mg/kg | | Administration: | Chronic treatment ; daily for 6 weeks | | Result: | Significantly increased the phosphorylated eNOS (Ser1177) and total eNOS but not the phosphorylated to total eNOS ratio in aortae of 18 weeks old ApoE?/? mice.
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| [References]
[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. DOI:10.1016/j.bmcl.2006.12.044
[2] Lin W, et al. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570. DOI:10.1371/journal.pone.0044570
[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. DOI:10.1111/j.1476-5381.2010.01158.x |
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