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FABP inhibitors bind fatty acid-binding proteins, small cytoplasmic carriers of long-chain fatty acids. Fatty acid-binding proteins (FABPs) are lipid chaperones with tissue-specific isoforms, such as FABP1 in liver, FABP3 in heart and FABP4 in adipocytes and macrophages. In 1996, mice lacking FABP4, then called adipocyte protein 2 (aP2), became obese on a high-fat diet without developing insulin resistance. BMS-309403 sodium is a salt of an FABP4 inhibitor that was studied in 2007 in mouse models of diabetes and atherosclerosis. HTS01037 and LDN-0088050 are listed as FABP4-directed inhibitors, while RO6806051 and FABP4/5-IN-6 inhibit both FABP4 and FABP5. FABP1-IN-1 and FABP-IN-2 extend the set to the liver and heart isoforms.
