BMS-309403 is a potent (Ki <2 nM FABP4, Ki = 250 nM FABP3, Ki = 350 nM FABP5) and selective inhibitor of the fatty-acid-binding protein aP2 (FABP4).1,2 It demonstrated marked reductions in atherosclerotic lesions in an Apoe-/- mouse model and improved glucose metabolism, reduced inflammation, and increased insulin sensitivity in a Lepob/ob mouse model. BMS-309403 stimulated glucose uptake in myotubes via activation of AMPK.3 It decreased ER stress-associated inflammation in skeletal muscle4 and suppressed inflammation and oxidative stress in mouse and cell models of acute lung injury5.
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