化合物SR 1664 T23389

Product Introduction
Bioactivity


英文名: SR1664

描述: SR1664 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。

体外活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/ml (109.57 mM)


关键字: Inhibitor | inhibit | HEK293T | F282 | SR1664 | clash | stereospecificity | PPAR | dependent | phosphorylation | SR-1664 | S273 | Peroxisome proliferator-activated receptors

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