SR1664

Research use only, not for human use.

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.

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.(In Vitro):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.

——

——

SR 1664

Metabolic Enzyme/Protease

PPAR

Reverse Transcriptase

——

——

1338259-05-4

547.611

C33H29N3O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (182.62 mM)

[H][C@@](C)(\N=C(/O)c1ccc2n(Cc3ccc(cc3)-c3ccccc3C(O)=O)c(C)c(C)c2c1)c1ccc(cc1)N(=O)=O

——

(-20℃)

With Ice Pack

≥ 2 years