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Filgotinib

CAS No. : 1206161-97-8

MCE 站：Filgotinib

产品活性：Filgotinib (GLPG0634) 是一种选择性的 JAK 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  |  Stem Cell/Wnt  |  JAK/STAT Signaling

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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-COVID-19 Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Gandotinib  |  Lestaurtinib  |  Oclacitinib maleate  |  JANEX-1  |  Cucurbitacin I  |  XL019  |  Atractylenolide I  |  FLLL32  |  Brevilin A  |  LFM-A13  |  Ginsenoside Rk1  |  ZM39923 hydrochloride  |  WHI-P154  |  Curculigoside  |  FM-381  |  RO8191  |  Reticuline  |  Ilginatinib maleate  |  TCS 21311  |  WHI-P97  |  Protosappanin A  |  Coumermycin A1  |  Dehydrocrenatidine  |  Delphinidin chloride  |  FM-479  |  NSC 33994

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