BMS-309403 sodium

Fatty acid binding protein 4 (FABP4) is a lipid transport protein that is also known as adipocyte FABP and aP2. In addition to adipocytes, it is also abundant in macrophages, along with FABP5, the epidermal FABP.¹ BMS309403 is a cell-permeable, potent inhibitor of FABP4 that targets the fatty acid-binding pocket (K_i < 2 nM).² It is less effective against FABP3 and FABP5 (K_is = 250 and 350 nM, respectively).² BMS309403 is orally active, reducing atherosclerosis in mice lacking apoplipoprotein E.^3,4 It also protects against the development of insulin resistance associated with genetic or diet-induced obesity in mice.^3,5 FABP4 dose-dependently suppresses the release of MCP-1 from macrophages.^1,5

1.Lan, H., Cheng, C.C., Kowalski, T.J., et al.Small-molecule inhibitors of FABP4/5 ameliorate dyslipidemia but not insulin resistance in mice with diet-induced obesityJ. Lipid Res.52(4)646-656(2011) 2.Sulsky, R., Magnin, D.R., Huang, Y., et al.Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP)Bioorg. Med. Chem. Lett.17(12)3511-3515(2007) 3.Furuhashi, M., Tuncman, G., G?rgün, C.Z., et al.Treatment of diabetes and atherosclerosis by inhibiting fatty-acid-binding protein aP2Nature447959-965(2007) 4.Lee, M.Y., Li, H., Xiao, Y., et al.Chronic administration of BMS309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cellsBr. J. Pharmacol.162(7)1564-1576(2011) 5.Suhre, K., R?misch-Margl, W., de Angelis, M.H., et al.Identification of a potential biomarker for FABP4 inhibition: The power of lipidomics in preclinical drug testingJ. Biomol. Screen.16(5)467-475(2011)