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RN486

CAS No. : 1242156-23-5

MCE 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，K_d 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.

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