HTS01037

Adipocyte fatty acid binding protein (A-FABP/aP2) is a carrier protein expressed in both adipocytes and macrophages where it functions in intracellular fatty acid solubilization, trafficking, and metabolism.¹ Molecular disruption of A-FABP/aP2 in mice results in improved insulin sensitivity and protection from atherosclerosis.^2,3 HTS 01037 is a high-affinity ligand of adipocyte fatty acid binding protein (A-FABP/aP2) (K_i = 0.67 μM) that presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2.⁴ At a concentration of 10 μM, HTS 01037 antagonizes the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes. ⁴ HTS 01037 inhibits lipolysis in 3T3L1 adipocytes and reduces lipopolysaccharide-stimulated inflammation in bone marrow-derived macrophages, both effects of which are similar to the phenotype of A-FABP/aP2 knockout mice.⁴

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