Identification | Back Directory | [Name]
Saroglitazar (Magnesium) | [CAS]
1639792-20-3 | [Synonyms]
Saroglitazar D4 Mg Salt Saroglitazar (Magnesium) magnesium (S)-2-ethoxy-3-(4-(2-(2-methyl-5-(4-(methylthio)phenyl)-1H-pyrrol-1-yl)ethoxy)phenyl)propanoate | [Molecular Formula]
C50H56MgN2O8S2 | [MDL Number]
MFCD29075338 | [MOL File]
1639792-20-3.mol | [Molecular Weight]
901.43 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (55.47 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. | [Biological Activity]
Potent and selective PPARα/γ agonist.
Saroglitazar is a potent and selective PPARα/γ (peroxisome proliferator-activated receptor) agonist th at exhibits lipid-lowering and insulin-sensitizing effects. Saroglitazar is approved in India for the treatment of diabetes type 2 and dyslipidemia. | [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 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 therapeutic agent for treatment of dyslipidemia and diabetes[1]. | [IC 50]
PPARα: 0.65 pM (EC50, HepG2 cell); PPARγ: 3 nM (EC50, HepG2 cell) | [References]
[1] Jain MR, et al. Saroglitazar, a novel PPARα/γ agonist with predominant PPARα activity, shows lipid-lowering effects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136. DOI:10.1002/prp2.136 |
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