BMS-309403, a substance used as an inhibitor of adipocyte fatty acid-binding protein, has been suggested as a new therapeutic agent for treating type 2 diabetes mellitus and atherosclerosis. Fatty acid binding proteins (FABPs) are small-molecular weight hydrophobic proteins containing a large hydrophobic cavity, into which naturally occurring long-chain fatty acids and synthetic hydrophobic ligands can be accepted. FABPs act as transporters of endogenous fatty acids from the cell surface to various sites of fatty acid storage and metabolism. In addition to the roles of FABP4 in regulating lipid metabolism and insulin sensitivity, recent pharmacological and biological findings have indicated a regulatory function of FABP4 in inflammation. FABP4 is expressed mainly to macrophages and inflammatory response. BMS-309403 competes with fatty acids for the binding pocket of A-FABP with high specificity. BMS-309403 is regarded as a lead compound for effective treatment of obesity related cardio-metabolic diseases. It also has off-target activity - it stimulates glucose uptake in C2C12 myotubes in a temporal and dose dependent manner via activation of AMP-activated protein kinase (AMPK) signaling pathway but independent of FABPs