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BTK inhibitor 17

CAS No. : 1858206-76-4

MCE 站：BTK inhibitor 17

产品活性：BTK inhibitor 17 是一种有效的具有口服活性不可逆 BTK 抑制剂，IC₅₀ 为 2.1 nM。BTK inhibitor 17 可用于类风湿关节炎的研究。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: BTK inhibitor 17 (compound 8) could covalently bind to Cys481 ａnd formed an HB network with hinge key residues Met477, Glu475, ａnd gatekeeper Thr474.

In Vivo: BTK inhibitor 17 (compound 8; 3-10 mg/kg; oral gavage; daily; for 28 days) treatment inhibits the significant progression of the disease ａnd exhibits a clear dose-dependent reduction per paw clinical scores, ａnd no significant body weight loss is observed for all different dosages.
BTK inhibitor 17 (compound 8) shows >95% plasma protein binding across three species of human, rat, ａnd mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), ａnd AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher C_max (rat, 466 ng/mL; mice, 252 ng/mL) ａnd plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%).

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Orally Active Compound Library  |  Anti-Blood Cancer Compound Library  |  Ibrutinib-biotin  |  CG-806  |  LFM-A13  |  Ibrutinib deacryloylpiperidine  |  PCI 29732  |  Acalabrutinib D4

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