Saroglitazar

495399-09-2

C25H29NO4S

DMSO : >= 25 mg/mL (56.87 mM); H2O : < 0.1 mg/mL (insoluble)

Cell Cycle/DNA Damage

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARalpha and moderate PPARgamma activity with EC₅₀ values of 0.65 pM and 3 nM in HepG2 cells, respectively. IC50 & Target: EC50: 0.65 pM (hPPARalpha, HepG2 cell); 3 nM (hPPARgamma, HepG2 cell)^[1] In Vivo: 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^[1].