| 产品描述: | 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. |
| 靶点: |
PPARα:0.65 pM (EC50, HepG2 cell);PPARγ:3 nM (EC50, HepG2 cell);Others |
| 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 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 |
| 参考文献: |
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. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.109 ml |
5.547 ml |
11.094 ml |
| 5 mM |
0.222 ml |
1.109 ml |
2.219 ml |
| 10 mM |
0.111 ml |
0.555 ml |
1.109 ml |
| 50 mM |
0.022 ml |
0.111 ml |
0.222 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |