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CAS No. : 1242156-23-5
MCE 国际站:RN486
产品活性:RN486 是一种有效的,选择性的,具有口服活性的 Btk 抑制剂,IC50 为 4.0 nM,Kd 为 0.31 nM,对其他激酶的活性较低。RN486 可用于类风湿关节炎和系统性红斑狼疮的研究。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:Btk
In Vitro: RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM).
In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486.
In Vivo: RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood.
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 | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Atuzabrutinib | PCI 29732 | JAK3/BTK-IN-6 | Pirtobrutinib | CNX-500 | BTK inhibitor 17 | Remibrutinib | GDC-0834 Racemate | Spebrutinib besylate | BTK inhibitor 19 | BMX-IN-1 | BMS-935177 | Ibrutinib | PF-06250112 | QL-X-138 | SJF620 hydrochloride | PROTAC BTK Degrader-2 | BTK-IN-8 | JAK3/BTK-IN-3 | JS25 | JAK3/BTK-IN-2 | (R)-Zanubrutinib | Edralbrutinib | Branebrutinib | Poseltinib | BTK inhibitor 20 | RET-IN-14 | QL47 | BTK-IN-23
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货号: HY-18018
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