PF429242 dihydrochloride 是一种可逆的竞争性SREBP位点 1 蛋白酶抑制剂,IC50值为175 nM。
产品描述
PF429242 dihydrochloride can reversibly inhibit S1P (IC50 of 175 nM).
体外活性
10 μM PF-429242 down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In HepG2 cells, PF-429242 inhibits cholesterol synthesis, with an IC50 of 0.5 μM[1]. PF-429242 treatment also shows suppressive effects on DENV2 yields in the cultured fluids of human-derived HEK-293, Hep G2, and non-human-primate derived LLC-MK2 cells[2]. PF-429242 has potent antiviral against LCMV and LASV [3].
体内活性
PF-429242 inhibits the expression of hepatic SREBP target genes, and the hepatic rates of cholesterol and fatty acid synthesis are reduced In mice[1].
Cas No.
2248666-66-0
分子式
C25H37Cl2N3O2
分子量
482.49
储存和溶解度
H2O:50 mg/mL (103.63 mM),Need ultrasonic
DMSO:83.3 mg/mL (165.81 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years