1338259-05-4

SR 1664 is a PPARγ non-agonist, which blocks Cdk5-mediated phosphorylation.

ChEBI: [1,1'-biphenyl]-2-carboxylic acid, 4'-[[2,3-dimethyl-5-[[[(1s)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1h-indol-1-yl]methyl]- is an indolecarboxamide.

SR1664 is a non-agonist PPARγ ligand and an inhibitor of Cdk5-mediated PPARγ phosphorylation. It has strong antidiabetic activity in two murine models of diabetes without the side effects normally asociated with the thiazolidinedione (TZD) antidiabetic PPARγ agonists. The TZD antidiabetics such as rosiglitazone and pioglitazone are full PPARγ agonistsbut recent data have suggested th at their separate activityinhibition of the the obesity-linked PPARγ phosphorylation by Cdk5is likely the more important activity for antidiabetic action. SR1664 has an IC50 of 80 nM in a competitive binding assayblocked the Cdk5-mediated phosphorylation of PPARγ in vitro with IC50 between 20 and 200 nM and exhibited no PPARγ agonist activity.