Saroglitazar-Magnesium - PPAR Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESaroglitazar MagnesiumCat. No.: HY-19937ACAS No.: 1639792-20-3分式: CHNOSMg分量: 901.42作靶點(diǎn): PPAR作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (55.47 mM; Nee

2、d ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (3.05 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (3.05 mM); Suspended solution; Need ultrasonic3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChe

3、mESolubility: 2.75 mg/mL (3.05 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Saroglitazar magnesium種新型的過(guò)氧化物酶體增殖物活化受體PPAR的激動(dòng)劑，具有顯著PPAR活性和中度PPAR活性，在HepG2細(xì)胞中的EC50值分別為0.65 pM and 3 nM。IC50 & Target PPAR PPAR0.65 pM (EC50, HepG2 cell) 3 nM (EC50, HepG2 cell)體內(nèi)研究 In db/db mice, 12-day treatment with Saroglita

4、zar (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 (91%) reduction in serum insulinand AUC-glucose following ora

5、l 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 humans. Based on efficacy and safety profile,Saroglitazar appear

6、s to have good potential as novel therapeutic agent for treatment of dyslipidemia anddiabetes 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% carb

7、oxymethylcellulose 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 carboxymethy

8、lcellulose) 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 ac

9、id (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 med