R112
目录号: PL11548 纯度: ≥99%
CAS No. :575474-82-7
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中文名称
R112
中文别名
3,3'-[(5-氟-2,4-嘧啶二基)二亚胺]二[苯酚];Phenol, 3,3'-[(5-fluoro-2,4-pyrimidinediyl)diimino]bis-
英文名称
R112
英文别名
Phenol, 3,3'-[(5-fluoro-2,4-pyrimidinediyl)diimino]bis-;3,3'-[(5-Fluoro-2,4-pyrimidinediyl)diimino]diphenol;R 112 (pharMaceutical);(E)-Elafibranor;TVKGTSHBQZEFEE-UHFFFAOYSA-N;BCP20695;BDBM50249090;AK547870;A14161;N2,N4-bis(3-hydroxyphenyl)-5-fluoro-2,4-primidinediamine;3,3''-(5-fluoropyrimidine-2,4-diyl)bis(azanediyl)diphenol;N2,N4-bis(3-hydroxyphenyl)-5-fluoro-2,4-pyrimidinediamine;3-[[5-fluoro-2-(3-hydroxyanilino)pyrimidin-4-yl]amino]phenol;3-({5-fluoro-4-[(3-hydroxyphenyl)amino]p;CID 9904854;R112
Cas No.
575474-82-7
分子式
C16H13FN4O2
分子量
312.30
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
R112 是一种快速且可逆的脾酪氨酸激酶 (Syk) 的激酶抑制剂。R112 抑制 Syk 激酶活性,IC50 值为 226 nM,Ki 值为 96 nM。R112 抑制 IgE-FcεRI 信号通路。R112 可用于过敏性鼻炎的研究。
生物活性
R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC 50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis.
性状
Solid
IC50 & Target[1][2]
IC50: 226 nM (Syk kinase)
体外研究(In Vitro)
R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC50s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC50 value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC50s of 0.115, 2.01, 1.58 and 1.75 μM, respectively.
R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Rossi AB, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-755.
溶解度数据
In Vitro: DMSO : 55 mg/mL (176.11 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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