Aleglitazar Inhibitor

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(R1439; RO-0728804) is a new dual PPAR-alpha/gamma agonist with IC50 of 2.8nM/4.6nM. IC50 Value: 2.8nM(PPAR-alpha); 4.6nM(PPAR-gamma) Target: PPARalpha/gamma Aleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARalpha and PPARgamma. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones. 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.

Benardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-alpha/gamma agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74.
Benardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-alpha/gamma agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74.
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.
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.
Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPARalpha/gamma agonist, has no clinically relevant pharmacokinetic interaction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12.
Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPARalpha/gamma agonist, has no clinically relevant pharmacokinetic interaction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12.
Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-alpha/gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-alpha/gamma agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16.
Benardeau 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.
Benardeau 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.

Small volumes of Aleglitazar, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5754494 is an inhibitor targeting Aleglitazar.