A PPARα and PPARγ dual agonist (EC50s = 0.65 and 3

Saroglitazar – 2.5 mg

Brand:
Cayman
CAS:
495399-09-2
Storage:
-20
UN-No:
Non-Hazardous - /

Saroglitazar 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 (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-α, IL-1β, and IL-6 expression 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 fibrosis in a mouse model of fibrosis induced by carbon tetrachloride.  

 

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Description

A PPARα and PPARγ dual agonist (EC50s = 0.65 and 3,000 pM, respectively); decreases serum triglyceride, free fatty acid, and glucose levels in a db/db mouse model of diabetes at 0.01-3 mg/kg; increases insulin sensitivity in an oral glucose challenge at 1 mg/kg; reverses palmitic acid-induced decreases in SOD1, SOD2, GPX, and catalase expression and increases in TNF-α, IL-1β, and IL-6 expression in HepG2 cells at 10 µM; decreases hepatic inflammation and steatosis in a mouse model of NASH induced by a choline-deficient high-fat diet at 3 mg/kg

Formal name: αS-ethoxy-4-[2-[2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrol-1-yl]ethoxy]-benzenepropanoic acid

Synonyms: 

Molecular weight: 439.6

CAS: 495399-09-2

Purity: ≥95%

Formulation: A neat oil

Product Type|Biochemicals|Ox Stress Reagents|Antioxidants||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Immunology & Inflammation

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