Chemical Name: 4'-[[2,3-Dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
Biological ActivityAntidiabetic agent; binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity. Does not inhibit Cdk5-dependent phosphorylation of Rb. Reduces fasting insulin levels and improves insulin sensitivity in a mouse model of diabetes.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
A second chance for a PPARγ targeted therapy?
Norris and Sigmund
Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation.
Choi et al.
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VersaClone cDNA Plasmids
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