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AS1517499

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Chemical Structure| 919486-40-1 同义名 : -
CAS号 : 919486-40-1
货号 : A290303
分子式 : C20H20ClN5O2
纯度 : 98%+
分子量 : 397.858
MDL号 : MFCD24038757
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(87.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.57mL

2.51mL

1.26mL

25.13mL

5.03mL

2.51mL
参考文献

[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.