S85541 |
Saroglitazar |
源叶(MedMol) | 97% |
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- 产品描述: Saroglitazar 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.
- 靶点: PPARα:0.65 pM (EC50, HepG2 cell);PPARγ:3 nM (EC50, HepG2 cell);PPAR
- 体内研究:
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
- 参考文献:
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.
- 溶解性: Soluble in DMSO
- 保存条件: -20°C
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.275 ml 11.375 ml 22.75 ml 5 mM 0.455 ml 2.275 ml 4.55 ml 10 mM 0.227 ml 1.137 ml 2.275 ml 50 mM 0.045 ml 0.227 ml 0.455 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)