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PF429242 dihydrochloride

CAS号

2248666-66-0

分子式

C25H37Cl2N3O2

主要靶点

S1P Receptor

仅限科研使用

Cat No : CM06531

Print datasheet

Synonyms

PF-429242|PF429242|PF429242 dihydrochloride|PF429242 Dihydrochloride|PF-429242 Dihydrochloride|PF-429242 dihydrochloride|PF 429242|PF 429242 Dihydrochloride|Inhibitor|Virus Protease|S1PReceptor|S1P|S1P Receptor|Fatty Acid Synthase (FASN)|inhibit

验证数据展示

  • CAS No.: 2248666-66-0

    PF429242 dihydrochloride
    CAS#: 2248666-66-0

产品信息

CAS号 2248666-66-0
分子式 C25H37Cl2N3O2
主要靶点 S1P Receptor
主要通路 G 蛋白偶联受体
分子量 482.49
纯度 98.67%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 PF-429242|PF429242|PF429242 dihydrochloride|PF429242 Dihydrochloride|PF-429242 Dihydrochloride|PF-429242 dihydrochloride|PF 429242|PF 429242 Dihydrochloride|Inhibitor|Virus Protease|S1PReceptor|S1P|S1P Receptor|Fatty Acid Synthase (FASN)|inhibit

靶点活性

S1P:175 nM

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].

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].

溶解度

H2O:50 mg/mL (103.63 mM);DMSO:83.3 mg/mL (165.81 mM)

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.

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