Remibrutinib ( LOU064 ) is a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase. Remibrutinib ( 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. It demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis. Remibrutinib ( LOU064 ) is currently being tested in phase 2 clinical studies for chronic spontaneous urticaria and Sjoegren’s syndrome.
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名称 | Remibrutinib ( LOU064 ) |
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Iupac 化学名称 | N-(3-(6-amino-5-(2-(N-methylacrylamido)ethoxy)pyrimidin-4-yl)-5-fluoro-2-methylphenyl)-4-cyclopropyl-2-fluorobenzamide |
同义词 | Remibrutinib ; LOU064 ; LOU 064 ; LOU-064 |
英文同义词 | Remibrutinib ; LOU064 ; LOU 064 ; LOU-064 |
分子式 | C27H27F2N5O3 |
分子量 | 507.53 |
Smile | O=C(NC1=CC(F)=CC(C2=NC=NC(N)=C2OCCN(C)C(C=C)=O)=C1C)C3=CC=C(C4CC4)C=C3F |
InChiKey | CUABMPOJOBCXJI-UHFFFAOYSA-N |
InChi | InChI=1S/C27H27F2N5O3/c1-4-23(35)34(3)9-10-37-25-24(31-14-32-26(25)30)20-12-18(28)13-22(15(20)2)33-27(36)19-8-7-17(11-21(19)29)16-5-6-16/h4,7-8,11-14,16H,1,5-6,9-10H2,2-3H3,(H,33,36)(H2,30,31,32) |
Cas号 | 1787294-07-8 |
相关CAS号 | 1787294-07-8 |
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