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Upadacitinib
CAS No. : 1310726-60-3
MCE 国际站：Upadacitinib
产品活性：Upadacitinib (ABT-494) 是一种高效的、具有口服活性的、选择性 Janus 激酶 1 (JAK1) 抑制剂 (IC50=43 nM)。Upadacitinib 对 JAK1 的选择性约为 JAK2 (200 nM）的 74 倍。Upadacitinib 可用于多种自身免疫性疾病的研究。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点：JAK
In Vitro: In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance). The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.
In Vivo: Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models.
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