Elafibranor

Elafibranor is an agonist of the peroxisome proliferator-activated receptors (PPAR) alpha and delta. It increases HDL secretion and expression of the lipid-related genes ABCA1, PLIN2, and ABHD5 in Caco-2/TC7 cells in a PPARalpha-dependent manner. Elafibranor (10 mg/kg) decreases levels of plasma triglycerides and total cholesterol while increasing plasma HDL and expression of Acox1, a PPARalpha target gene, in the liver of ApoE2-KI wild-type, but not PPARalpha knockout, mice fed a Western diet. However, PPARalpha knockout mice exhibit a decrease in plasma total and non-HDL cholesterol levels, indicating PPARdelta has a role in these functions. Elafibranor (30 mg/kg) reduces diet-induced macro- and micro-steatosis in a PPARalpha-deficient mouse model of non-alcoholic steatohepatitis. It also reduces cholesterol and triglyceride accumulation as well as macrovesicular steatosis in the liver of insulin-resistant db/db mice fed the methionine-choline deficient (MCD) diet. Formulations containing elafibranor are under clinical investigation for the treatment of non-alcoholic steatohepatitis.Formal Name: 2-[2,6-dimethyl-4-[(1E)-3-[4-(methylthio)phenyl]-3-oxo-1-propen-1-yl]phenoxy]-2-methyl-propanoic acid. CAS Number: 923978-27-2. Synonyms: GFT505. Molecular Formula: C22H24O4S. Formula Weight: 384.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble, Methanol: Slightly Soluble. SMILES: CSC1=CC=C(C(/C=C/C2=CC(C)=C(OC(C)(C)C(O)=O)C(C)=C2)=O)C=C1. InChi Code: InChI=1S/C22H24O4S/c1-14-12-16(13-15(2)20(14)26-22(3,4)21(24)25)6-11-19(23)17-7-9-18(27-5)10-8-17/h6-13H,1-5H3,(H,24,25)/b11-6+. InChi Key: AFLFKFHDSCQHOL-IZZDOVSWSA-N.