Filgotinib,1206161-97-8

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Filgotinib

CAS No. : 1206161-97-8

MCE 国际站：Filgotinib

产品活性：Filgotinib (GLPG0634) 是一种选择性的，具有口服活性的 JAK1 抑制剂，能够有效抑制 JAK1，JAK2，JAK3 和 TYK2 的活性，IC₅₀ 值分别为 10 nM，28 nM，810 nM 和 116 nM。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：JAK

In Vitro: Filgotinib (GLPG0634) dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. Filgotinib also inhibits Th1 differentiation with similar potencies of 1 μM or lower. Filgotinib (GLPG0634)?does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC₅₀ > 10 μM).

In Vivo: Filgotinib (GLPG0634; 3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. Filgotinib (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3⁺ cells) and macrophages (F4/80⁺ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1. Filgotinib (GLPG0634; 0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model.

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