Saroglitazar - PPAR Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESaroglitazarCat. No.: HY-19937CAS No.: 495399-09-2分式: CHNOS分量: 439.57作靶点: PPAR作通路: Cell Cycle/DNA Damage储存式: Pure form -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL (56.87 mM)H2O : 40% PEG30

2、0 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.69 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Saroglitazar种新型的过氧化物酶体增殖物活化受体PPAR的激动剂，具有显著PPAR活性和中度PPAR活性, 在HepG2细胞中的EC50值分别为0.65 pM and 3 nM。IC50 & Target PPAR PPAR0.65 pM (EC50, HepG2 cell) 3 nM (EC50, H

3、epG2 cell)体内研究 In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependentreductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects isfound to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant

4、(91%) reduction in serum insulinand AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dosecomparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar andhas indicated low risk of PPAR-associated side effects in hum

5、ans. Based on efficacy and safety profile,Saroglitazar appears to have good potential as novel 1.PROTOCOLAnimal Rats: Rats randomize based on body weights and are divided into three equal groups and receives the dailyAdministration 1 administration of vehicle (50% w/v honey for marmoset and 0.1% car

6、boxymethylcellulose for Wistar rats) orSaroglitazar (1.5 and 15 mg/kg per day) for 90 days by oral gavage 1.Mice: Male C57BL/6J-db/db mice are bled on day 0 to determine pretreatment serum glucose and TG.During next 12 days, each animal is dosed (by oral gavage) with vehicle (0.5% sodium carboxymeth

7、ylcellulose) or Saroglitazar (0.01, 0.03, 0.1, 0.3,1, and 3 mg/kg per day) or pioglitazone (60 mg/kg per day) andon day 12 of the treatment, blood samples are collected (1 h after dosing) from orbital sinus under light etheranesthesia. The serum is isolated and analyzed for glucose, TG, free fatty a

8、cid (FFA), and insulin levels 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jain MR, et al. Saroglitazar, a novel PPAR/ agonist with predominant PPAR activity, shows lipid-lowering and insulin-sensitizingeffects in preclinical models. Pharmacol Res Perspect. 2015 Jun;3(3):e00136.McePdfHeightCaution: Product has not been fully validated for medical applicatio