Formulation: A solid
Formal Name: (T-4)-bis[(αS)-α-(ethoxy-κO)-4-[2-[2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrol-1-yl]ethoxy]benzenepropanoato-κO]-magnesium
Purity: ≥98%
Formula Markup: C50H56MgN2O8S2
Formula Weight: 901,4
Shelf life (days): 1460
CAS Number: 1639792-20-3
Notes: Saroglitazar magnesium is a dual agonist of PPARα and PPARγ (EC50s = 0.65 and 3,000 pM, respectively, in a transactivation assay in HepG2 cells).{49145} 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 magnesium (10 µM) reverses palmitic acid-induced decreases in the expression of mRNA encoding superoxide dismutase 1 (SOD1), SOD2, glutathione peroxidase (GPX), and catalase and increases in the expression of mRNA encoding TNF-α, IL-1β, and IL-6 in HepG2 cells.{49146} 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 hepatic fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.
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