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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 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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