| 产品描述： | BTK抑制剂;BTK Inhibitors;;InformationRemibrutinib (LOU064) 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.TargetsBTK (Cell-free assay); IL-8 (Cell-free assay); CD69 (Cell-free assay) 1.3 nM; 2.5 nM; 18 nMIn vitroLOU064 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.In vivoLOU064 demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.Cell Research(from reference)Cell lines：human monocytic cell line THP1, Human Blood B cell and Basophil. Concentrations：3 nM, 10 nM, 30 nM, 100 nM, 300 nM Incubation Time：25 min, 50 min, 75 min, 100 min |
上海工商
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营业执照(三证合一)
北京