Remibrutinib (Synonyms: LOU064)
目录号: PL02968 纯度: ≥98%
CAS No. :1787294-07-8
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中文名称
Remibrutinib
英文名称
Remibrutinib
英文别名
Remibrutinib;I7MVZ8HDNU;remibrutinib (proposed INN);LOU064;GTPL10457;example 6 [WO2015079417A1];compound 25 [PMID: 32083858];US9512084, 6;N-(3-(6-Amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide;N-[3-[6-amino-5-[2-[methyl(prop-2-enoyl)amino]ethoxy]pyrimidin-4-yl]-5-fluoro-2-methylphenyl]-4-cyclopropyl-2-fluorobenzamide
Cas No.
1787294-07-8
分子式
C27H27F2N5O3
分子量
507.53
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Remibrutinib 是一种具有口服有效活性的 bruton tyrosine kinase (BTK) 抑制剂,IC50 值为 1 nM,在血液中抑制 BTK 活性的 IC50 的值为 0.23 μM。Remibrutinib 具有研究慢性荨麻疹 (CU) 的潜力。
生物活性
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC 50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC 50 value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.
性状
Solid
IC50 & Target[1][2]
IC50: 1 nM (BTK)
体外研究(In Vitro)
In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM.
In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC50 value of 0.023 μM, the whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats.
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
ClinicalTrial
参考文献
[1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1.
[2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23.
溶解度数据
In Vitro: DMSO : 125 mg/mL (246.29 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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