您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > PF429242 dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PF429242 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF429242 dihydrochloride图片
CAS NO:2248666-66-0
规格:98%
分子量:482.49
包装与价格:
包装价格(元)
200mg电议
500mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PF429242 dihydrochloride是可逆的,竞争性的S1P抑制剂,IC50值为175 nM。
CAS:2248666-66-0
分子式:C25H37Cl2N3O2
分子量:482.49
纯度:98%
存储:Store at -20°C

Background:

PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.


10 μM PF-429242 inhibits endogenous SREBP processing in Chinese hamster ovary cells. PF-429242 also 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]. The addition of PF-429242 (30 μM) shows statistically significant suppression of infectious viral titers and viral RNA copies in the cell culture fluids. 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 efficiently prevents the processing of GPC from the prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV, which correlates with the compound's potent antiviral activity against LCMV and LASV in cultured cells[3].


In mice treated with PF-429242 for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced[1].


参考文献:
[1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol Exp Ther. 2008 Sep;326(3):801-8.
[2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046.
[3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803.