Saroglitazar

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型 PPAR 激动剂，具有主要的 PPARα 活性和中等的 PPARγ 活性，EC50 分别为 0.65 pM 和 3 nM。

A novel PPAR agonist with predominant PPARα and moderate PPARγ activity with EC50 of 0.65 pM and 3 nM respectively; has been developed for the treatment of dyslipidaemia and has favourable effects on glycaemic parameters in type 2 diabetes mellitus.Diabetes Approved.

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In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel.

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Metabolic Enzyme/Protease

PPAR

PPAR

Metabolic Disease

Diabetes

495399-09-2

439.567

C25H29NO4S

>98% (HPLC)

DMSO: 10 mM

CCOC(CC1=CC=C(C=C1)OCCN2C(=CC=C2C3=CC=C(C=C3)SC)C)C(=O)O

Benzenepropanoic acid, α-ethoxy-4-[2-[2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrol-1-yl]ethoxy]-, (αS)-

(-20℃)

With Ice Pack

≥ 2 years