Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
説明 | 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. |
ターゲット&IC50 | PPARγ:28.67 nM(Ki), PPARγ:80 nM |
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[1]. |
別名 | SR 1664 |
分子量 | 547.6 |
分子式 | C33H29N3O5 |
CAS No. | 1338259-05-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/ml (109.57 mM)
You can also refer to dose conversion for different animals. 詳細
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SR1664 1338259-05-4 DNA Damage/DNA Repair Metabolism PPAR Inhibitor inhibit HEK293T F282 clash SR 1664 stereospecificity dependent phosphorylation SR-1664 S273 Peroxisome proliferator-activated receptors inhibitor