HTS01037 is a fatty acid-binding inhibitor and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 (Ki: 0.67 μM).

AFABP/aP2:0.67 μM

HTS01037 inhibits lipolysis in 3T3-L1 adipocytes and decreases LPS-stimulated inflammation in cultured macrophages. HTS01037 functions as a high affinity ligand of AFABP/aP2 (apparent Ki: 0.67 μM). HTS01037 is somewhat selective for AFABP/aP2, but at higher concentrations is a pan-specific FABP inhibitor. Treatment of microglial cells with HTS01037 enhances expression of Ucp2 and arginase in the presence or absence of palmitic acid. 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]. Cells exposed to HTS01037 shows attenuated expression of inducible nitric oxide synthase (iNOS) compared to palmitic acid alone indicating reduced NFκB signaling[2]. Treatment of macrophages with HTS01037 causes a marked decrease in both basal and fatty acid-stimulated LTC4 secretion but no change in 5-HETE production or 5-lipoxygenase expression[3].