货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T92602-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T92602-1ml ￥648.00 现货	4 4	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T92602-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

S1P 受体抑制剂;S1P Receptor Inhibitors;;InformationPF 429242 PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).TargetsS1P (Cell-free assay) 170 nMIn vitroIn cultured human liver (Hep-G2) cells, PF-429242 prevents proteolytic processing and nuclear translocation of SREBP, reduces the expression of key genes involved in cholesterol synthesis and fatty acid synthesis, and inhibits both pathways in the absence of any cytotoxicity. The addition of PF-429242 suppresses the viral propagation of all serotypes of DENV in several primate-derived cells.In vivoPK data for PF-429242 show that it had rapid clearance (CL = 75 ml/min/kg) and poor oral bioavailability (5%) in rats.Cell Research(from reference)Cell lines：HeLa cells Concentrations：3 to 300 µM Incubation Time：72 h

体内研究：

在用 PF-429242 处理 24 h 的小鼠中，肝脏 SREBP 靶基因的表达受到抑制，肝脏胆固醇和脂肪酸合成率降低。

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.
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.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.442 ml	12.208 ml	24.415 ml
5 mM	0.488 ml	2.442 ml	4.883 ml
10 mM	0.244 ml	1.221 ml	2.442 ml
50 mM	0.049 ml	0.244 ml	0.488 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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