Saroglitazar

Saroglitazar is a dual agonist of PPARalpha and PPARgamma (EC50s = 0.65 and 3,000 pM, respectively, in a transactivation assay in HepG2 cells). It decreases serum triglyceride, free fatty acid, and glucose levels in a db/db mouse model of diabetes when administered at doses ranging from 0.01 to 3 mg/kg per day for 12 days. It increases insulin sensitivity in an oral glucose challenge when administered at a dose of 1 mg/kg in db/db mice, as well as decreases LDL levels in hApoB100/hCETP mice and in hamsters fed a high-fat high-cholesterol diet. Saroglitazar (10 µM) reverses palmitic acid-induced decreases in the expression of superoxide dismutase 1 (SOD1), SOD2, glutathione peroxidase (GPX), and catalase and increases in TNF-alpha, IL-1beta, and IL-6 expression in HepG2 cells. It decreases hepatic inflammation and steatosis in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a choline-deficient high-fat diet when administered at a dose of 3 mg/kg and inhibits fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.Formal Name: alphaS-ethoxy-4-[2-[2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrol-1-yl]ethoxy]-benzenepropanoic acid. CAS Number: 495399-09-2. Molecular Formula: C25H29NO4S. Formula Weight: 439.6. Purity: >90%. Formulation: (Request formulation change), A neat oil. Solubility: Chloroform: slightly soluble, Methanol: slightly soluble. SMILES: OC([C@@H](OCC)CC1=CC=C(OCCN2C(C)=CC=C2C3=CC=C(SC)C=C3)C=C1)=O. InChi Code: InChI=1S/C25H29NO4S/c1-4-29-24(25(27)28)17-19-6-10-21(11-7-19)30-16-15-26-18(2)5-14-23(26)20-8-12-22(31-3)13-9-20/h5-14,24H,4,15-17H2,1-3H3,(H,27,28)/t24-/m0/s1. InChi Key: MRWFZSLZNUJVQW-DEOSSOPVSA-N.