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Submit ReviewAS 1517499 is a potent STAT6 inhibitor (IC50 = 21 nM). In vitro, it inhibits IL-4-induced Th2 differentiation of mouse spleen T cells (IC50 = 2.3 nM), without influencing Th1 differentiation induced by IL-12. In a mouse model of allergic bronchial asthma, treatment with AS 1517499 reduces mouse airway IL-3 production and partly inhibits the RhoA upregulation in bronchial smooth muscles.
分子量 | 397.86 |
公式 | C20H20ClN5O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 919486-40-1 |
PubChem ID | 10340781 |
InChI Key | OZRMEKAUZBKTTC-UHFFFAOYSA-N |
Smiles | O=C(N)C1=CN=C(N=C1NCC=2C=CC=CC2)NCCC3=CC=C(O)C(Cl)=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.89 | 50 | |
ethanol | 3.98 | 10 |
以下数据基于产品分子量 397.86。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 5.03 mL | 25.13 mL | 50.27 mL |
2.5 mM | 1.01 mL | 5.03 mL | 10.05 mL |
5 mM | 0.5 mL | 2.51 mL | 5.03 mL |
25 mM | 0.1 mL | 0.5 mL | 1.01 mL |
参考文献是支持产品生物活性的出版物。
Chiba et al (2009) A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am.J.Respir.Cell Mol.Biol. 41 516 PMID: 19202006
Nagashima et al (2008) Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine- 5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Bioorg.Med.Chem. 16 6509 PMID: 18534856
Nagashima et al (2007) Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg.Med.Chem. 15 1044 PMID: 17071093
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关键词: AS 1517499, AS 1517499 supplier, AS1517499, STAT6, inhibitors, inhibits, In, vivo, potent, asthma, STAT, 7636, Tocris Bioscience
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