BMS-309403 sodium 是一种有效的选择性脂肪细胞脂肪酸结合蛋白aFABP, 也称为FABP4，aP2抑制剂，对 FABP4，FABP3 和 FABP5 的Ki分别为<2 nM，250 nM，350 nM。BMS-309403 sodium 与蛋白质内部的脂肪酸结合口袋相互作用，竞争性地抑制内源性脂肪酸的结合。BMS-309403 sodium 可改善载脂蛋白E缺乏症小鼠和培养的人内皮细胞的内皮功能。

BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with K i s 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]. 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.

C31H25N2NaO3

496.53

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years