HTS 01037

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. Molecular disruption of A-FABP/aP2 in mice results in improved insulin sensitivity and protection from atherosclerosis. HTS 01037 is a high-affinity ligand of adipocyte fatty acid binding protein (A-FABP/aP2) (Ki = 0.67 µM) that presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2. 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. 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.Formal Name: 4-[(3-carboxy-1-oxo-2-propen-1-yl)amino]-[2,2'-bithiophene]-5-carboxylic acid, 5-methyl ester. CAS Number: 682741-29-3. Molecular Formula: C14H11NO5S2. Formula Weight: 337.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml. lambdamax: 331 nm. SMILES: O=C(/C=C/C(O)=O)NC1=C(C(OC)=O)SC(C2=CC=CS2)=C1. InChi Code: InChI=1S/C14H11NO5S2/c1-20-14(19)13-8(15-11(16)4-5-12(17)18)7-10(22-13)9-3-2-6-21-9/h2-7H,1H3,(H,15,16)(H,17,18)/b5-4+. InChi Key: GJODSFZNKNHKML-SNAWJCMRSA-N.