HTS01037

HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a K_i of 0.67 μM. IC50 & Target: IC50: 0.67 μM (AFABP/aP2)^[1] In Vitro: HTS01037 functions as a high affinity ligand of AFABP/aP2 with an apparent K_i of 0.67 μM. HTS01037 is somewhat selective for AFABP/aP2, but at higher concentrations is a pan-specific FABP inhibitor. HTS01037 inhibits lipolysis in 3T3-L1 adipocytes and reduces LPS-stimulated inflammation in cultured macrophages. HTS01037 acts as an antagonist of the protein-protein interaction between AFABP/aP2 and hormone sensitive lipase but does not activate PPARγ in macrophage or CV-1 cells^[1]. Treatment of microglial cells with HTS01037 increases expression of Ucp2 and arginase in the presence or absence of palmitic acid. Moreover, cells exposed to HTS01037 exhibits attenuated expression of inducible nitric oxide synthase (iNOS) compared to palmitic acid alone indicating reduced NFκB signaling^[2]. Treatment of macrophages with HTS01037results in a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression^[3].