Aleglitazar-R1439-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAleglitazarCat. No.: HY-14728CAS No.: 475479-34-6Synonyms: R1439; RO0728804分式: CHNOS分量: 437.51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 (11

2、4.28 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.71 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.71 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Aleglitazar(R1439; RO-0728804)是PPAR-/激動(dòng)劑，IC50分別為2.8

3、nM/4.6 nM。IC50 & Target PPAR PPAR19 nM (IC50) 38 nM (IC50)REFERENCES1. Bnardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-/ agonist aleglitazar on glycaemic control and organ protection inthe Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74.2. Younk LM, Uhl L, Da

4、vis SN. Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with highcardiovascular risk. Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):753-63.3. Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPAR/ agonist, has no clinically relevant

5、pharmacokineticinteraction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12.4. Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-/ agonist: implications for cardiovascular disease inpatients with diabetes mellitus. Am J Cardiov

6、asc Drugs. 2010;10(4):209-16.5. Bnardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment oftype II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-82