BMS-309403 (BMS309403)是芳香联苯三唑化合物,是细胞渗透性的FABP4选择性抑制剂,Kd值为4 nM,对FABP3/4/5的Ki值分别为250 nM、<2 nM和350 nM。FABPs是内源性脂肪酸的转运体,将脂肪酸从细胞表面运送到脂肪酸储存和代谢的不同位点,而BMS-309403竞争性结合FABPs蛋白质内部结合脂肪酸的口袋。
参考文献
1.Sulsky R, et al. Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5.
2.Furuhashi M, et al. Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2. Nature. 2007 Jun 21;447(7147):959-65.
3.Lin W, et al. BMS309403 stimulates glucose uptake in myotubes through activation of AMP-activated protein kinase. PLoS One. 2012;7(8):e44570.
4.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 Apr;162(7):1564-76.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。





