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 具有治疗慢性荨麻疹 (CU) 的潜力。
货号:ajcx14708
CAS:1787294-07-8
分子式:C27H27F2N5O3
分子量：507.53
溶解度:DMSO: 125 mg/mL (246.29 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2].

In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM[1].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[1].

[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.