GW7647 是一种PPARα有效激动剂,对人 PPARα、PPARγ 和 PPARδ 的EC50值分别为 6、1.1 和 6.2 μM。
产品描述
GW7647 is a potent agonist of PPARα (EC50s: 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ, and PPARδ, respectively).
体外活性
GW7647 (50 nM) stimulates the PI3K phosphorylation followed by the Akt (Ser473) phosphorylation, which causes NOS1 phosphorylation increased the amounts of NO released in the stripped antral mucosa. GW7647 (50 nM) enhances the initial phase of Ca2+-regulated exocytotic events stimulated by ACh in antral mucous cells, but GW7647 alone does not evoke any exocytotic event. GW7647 (1 μM) induces a significant increase of PDZK1 protein expression to 129.7 ± 6.5% of vehicle treated control in Caco2BBE cells in the absence and presence of IL-1β. GW7647 also decreases the IL-1β-mediated decrease in PDZK1 expression[1]. GW7647 plus ACh stimulates the effects of wortmannin (50 nM) and AKT-inh (100 nM) on the exocytotic events in antral mucous cells[2]. GW 7647 (100 nM) decreases the AQP9 protein abundance by 43%, but it displays not significant effect at 10 and 1,000 nM in WIF-B9 hepatocytes. GW 7647 (100 nM) reduces a 24% reduction in AQP9 protein abundance in HepG2 cells, however, it does not significantly enhance the protein abundance of L-FABP in HepG2 hepatocytes[3].
体内活性
GW7647 (3 mg/kg per day) does not avoid the development of cardiac hypertrophy. It prevents the decline in left ventricular ejection fraction in vivo[4].
Cas No.
265129-71-3
分子式
C29H46N2O3S
分子量
502.75
别名
2-[[4-[2-[[环己基氨基)羰基](4-环己基丁基)氨基]乙基]苯基]硫基]-2-甲基丙酸
储存和溶解度
DMSO:60 mg/mL (119.34 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years