CAS NO: | 475479-34-6 |
包装: | 5mg |
市场价: | 7650元 |
Cas No. | 475479-34-6 |
别名 | 阿格列扎; R1439; RO0728804 |
Canonical SMILES | CC1=C(CCOC2=CC=C(C[C@@H](C(O)=O)OC)C3=C2C=CS3)N=C(C4=CC=CC=C4)O1 |
分子式 | C24H23NO5S |
分子量 | 437.51 |
溶解度 | DMSO: ≥ 50 mg/mL (114.28 mM); Water:< 0.1 mg/mL (insoluble) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones. PPARγ|19 nM (IC50)|PPARα|38 nM (IC50) [1]. BÉnardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-α/γ agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74. [2]. Younk LM, Uhl L, Davis SN. Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular 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 PPARα/γ agonist, has no clinically relevant pharmacokinetic interaction 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-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16. [5]. BÉnardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. |