| Description | Saroglitazar Magnesium is a novel peroxissome proliferator-activated receptor (PPAR) agonist with significant activation activity against PPARα (EC50 0.65pM) and moderate activation against PPARγ (EC50 3 nM). |
| In vivo | 在db/db小鼠中，Saroglitazar（每天0.01-3 mg/kg，口服）12天的治疗导致血清甘油三酯（TG）、游离脂肪酸（FFA）和葡萄糖水平的剂量依赖性降低。这些效应的ED50分别为0.05、0.19和0.19 mg/kg，且在1 mg/kg剂量下口服葡萄糖后，血清胰岛素和AUC-葡萄糖显著降低（分别为91%和59%）。在Wistar大鼠和狨猴中，一项为期90天的重复剂量比较研究证实了Saroglitazar的疗效（降低TG）潜力，并表明其在人体中有低PPAR相关副作用的风险。基于其疗效和安全性，Saroglitazar被认为是治疗血脂异常和糖尿病的新型潜在治疗剂。[1] |
| Target activity | PPARγ:3 nM （EC50， HepG2 cell）, PPARα:0.65 pM （EC50， HepG2 cell） |
| molecular weight | 901.43 |
| Molecular formula | C50H56MgN2O8S2 |
| CAS | 1639792-20-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 112.5 mg/mL (124.8 mM), Sonication is recommended. |
| References | 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. |