GW 6471 是 PPARα 的拮抗剂,IC50 为 0.24 μM。它增强 PPAR α 配体结合结构域与共抑制蛋白 SMRT 和 NCoR 的结合亲和力。
半岛bd体育手机客户端 描述
GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.
体外活性
A specific PPARα antagonist, GW6471, induced both apoptosis and cell cycle arrest at G0/G1 in VHL(+) and VHL(-) RCC cell lines (786-O and Caki-1) associated with attenuation of the cell cycle regulatory proteins c-Myc, Cyclin D1, and CDK4;?this data was confirmed as specific to PPARα antagonism by siRNA methods.
Cas No.
880635-03-0
分子式
C35H36F3N3O4
分子量
619.685
别名
GW 6471
储存和溶解度
DMSO:120 mg/mL (193.65 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years