PF-05221304

PF-05221304 is an inhibitor of acetyl-CoA carboxylase 1 (ACC1) and ACC2 (IC50s = 12.4 and 8.7 nM, respectively). It inhibits de novo lipid synthesis (IC50 = 61 nM) and increases fatty acid oxidation in primary human hepatocytes. PF-05221304 reduces the accumulation of triglycerides composed of de novo-derived fatty acids but not dietary essential fatty acids in primary human hepatocytes. In vivo, PF-05221304 (10 and 100 mg/kg) reduces hepatic malonyl-CoA production and de novo lipogenesis in rats. It reduces hepatic fibrosis, alanine transaminase (ALT) and aspartate aminotransferase (AST) levels, and triglyceride accumulation in a rat model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient and high-fat diet (CDAHFD).Formal Name: 4-[6-methoxy-4-[[1,4,6,7-tetrahydro-1-(1-methylethyl)-7-oxospiro[5H-indazole-5,4'-piperidin]-1'-yl]carbonyl]-2-pyridinyl]-benzoic acid. CAS Number: 1370448-25-1. Synonyms: Clesacostat. Molecular Formula: C28H30N4O5. Formula Weight: 502.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 255, 311 nm. SMILES: O=C(C1=CC=C(C2=CC(C(N3CCC4(CC3)CC(C5=C(C4)C=NN5C(C)C)=O)=O)=CC(OC)=N2)C=C1)O. InChi Code: InChI=1S/C28H30N4O5/c1-17(2)32-25-21(16-29-32)14-28(15-23(25)33)8-10-31(11-9-28)26(34)20-12-22(30-24(13-20)37-3)18-4-6-19(7-5-18)27(35)36/h4-7,12-13,16-17H,8-11,14-15H2,1-3H3,(H,35,36). InChi Key: LXZMHBHEXAELHH-UHFFFAOYSA-N.