|4-(苄氨基)-2-((3-氯-4-羟基苯乙基)氨基)嘧啶-5-甲酰胺|CsnPharm

CAS No.: 919486-40-1

AS1517499 Catalog No. CSN13598

Synonyms: AS-1517499

AS-1517499 is a potent STAT6 inhibitor with IC50 of 21 nM.

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实验方案

技术信息

生物活性

描述STAT6 (signal transducers and activators of transcription 6) protein is activated by IL-4 and IL-13, and plays an important role in Th2 cells (T-helper cell 2) differentiation, which might make it an excellent therapeutic target for various allergic conditions, including asthma and atopic diseases. AS1517499 is a STAT6 inhibitor with IC50 value of 21nM, and also inhibited IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM, but has no effect on the ability of spleen T cells to produce IFN-γ, which is a marker of Th1 differentiation. AS1517499 could inhibit IL-13–induced activation of STAT6 and up-regulation of RhoA in cultured hBSMCs at concentration of 100nM. Intraperitoneal injections of AS1517499 at dose of 10mg/kg 1h before each exposure to ovalbumin could almost completely inhibit both the antigen-induced up-regulation of RhoA and bronchial smooth muscle hyperresponsiveness in mice.
动物研究
剂量
Mice: 1 mg/kg, 10 mg/kg^[1] (i.p.), 20 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 1 mg/kg, 10 mg/kg^[1] (i.p.), 20 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Chiba Y, Todoroki M, et al. A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am J Respir Cell Mol Biol. 2009 Nov;41(5):516-24.
[2] Nagashima S, Yokota M, et al. Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl] amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg Med Chem. 2007 Jan 15;15(2):1044-55. Epub 2006 Oct 27.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5135 mL
- 12.5673 mL
- 25.1346 mL
- 5 mM
- 0.5027 mL
- 2.5135 mL
- 5.0269 mL
- 10 mM
- 0.2513 mL
- 1.2567 mL
- 2.5135 mL

技术信息

CAS号

919486-40-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H20ClN5O2

运输

蓝冰

分子量

397.86

别名

AS-1517499

溶解度

DMSO	79.0 mg/mL (198.6 mM)
Water	Insoluble
Ethanol	35.0 mg/mL (88.0 mM)

动物实验配方

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