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  • Remibrutinib
Remibrutinib的可视化放大

Remibrutinib

Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite

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Remibrutinib的二维码
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  • 5mg
    ¥2825.00
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  • 10mg
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  • 50mg
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  • 货号: ajcx14708
  • CAS: 1787294-07-8
  • 别名:
  • 分子式: C27H27F2N5O3
  • 分子量: 507.53
  • 纯度: >98%
  • 溶解度: DMSO: 125 mg/mL (246.29 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Remibrutinib (LOU064) is a potent, highly selective covalent inhibitor of bruton tyrosine kinase (BTK) with IC50 of 1.3 nM, 2.5 nM and 18 nM for BTK, FcγR-induced IL8 and anti-IgM/IL4-induced CD69, respectively. Remibrutinib (LOU064) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for the treatment of autoimmune diseases.


LOU064 exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases.[1]


LOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.[1]


[1] Daniela Angst, et al. J Med Chem. 2020 May 28;63(10):5102-5118.

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