Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.

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Benardeau A, Benz J, Binggeli A, Blum D, Boehringer M, Grether U, Hilpert H, Kuhn B, Marki HP, Meyer M, Puntener K, Raab S, Ruf A, Schlatter D, Mohr P

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. doi: 10.1016/j.bmcl.2009.03.036. Epub 2009 Mar 14.

PubMed ID
19349176 [ View in PubMed
]
Abstract

Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Peroxisome proliferator-activated receptor alphaQ07869Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AleglitazarPeroxisome proliferator-activated receptor alphaIC 50 (nM)38N/AN/ADetails
AleglitazarPeroxisome proliferator-activated receptor alphaEC 50 (nM)50N/AN/ADetails
AleglitazarPeroxisome proliferator-activated receptor gammaIC 50 (nM)19N/AN/ADetails
AleglitazarPeroxisome proliferator-activated receptor gammaEC 50 (nM)21N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaIC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)450N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)450N/AN/ADetails