HTS01037

Biochem/physiol Actions

HTS01037 is a selective, high-affinity fatty acid-binding protein FABP4 (AFABP; aP2) antagonist (aP2 Ki = 0.67 µM; EFABP/HF/IFABP/LFABP Ki = 3.40/9.07/6.57/8.17 µM) that targets aP2 long-chain fatty acid-binding site. HTS01037 is shown to downregulate basal and fatty acid-stimulated LTC4 levels in primary murine peritoneal macrophages (0.2-20 µM), upregulate murine macrophage RAW 264.7 intracellular free fatty acids and uncoupling protein 2 (UCP2) mRNA levels (30 µM), as well as suppress PPARγ target genes expression in IL-4 polarized human primary macrophages (10-25 µM).