Saroglitazar是一种新型的过氧化物酶体增殖物活化受体PPAR的激动剂，具有显著PPARα活性和中度PPARγ活性, 在HepG2细胞中的EC₅₀值分别为0.65 pM and 3 nM。

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC 50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

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PPARα 0.65 pM (EC50, HepG2 cell) PPARγ 3 n

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 ED 50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Jain MR, et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering and insulin-sensitizing effects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136.

In Vitro: DMSO : ≥ 25 mg/mL (56.87 mM)配制储备液