SR 1664是一种PPARγ拮抗剂，与结合PPARγ，可有效抑制 CDK5 介导的PPARγ磷酸化，IC50为80 nM，Ki为 28.67 nM。

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Mutagenesis of F282 to alanine (F282A) altered the pharmacology of SR1664 on PPARγ activity, acting as an agonist of the mutant receptor in a transcriptional activity assay, and differentially displacing nuclear receptor co-repressor 1. Together these results suggest that SR1664 actively antagonizes PPARγ through a stereo-specific AF2-mediated, F282-dependent clash, and that stereospecificity confers antagonism within the biaryl indole scaffold[1].

1338259-05-4

C33H29N3O5

547.6

SR 1664

DMSO:60 mg/ml (109.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years