产品
编 号:F115865
分子式:C17H19F3N6O
分子量:380.37
产品类型
结构图
CAS No: 1310726-60-3
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产品详情
生物活性:
Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research.
体内研究:
Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models.Animal Model:Female Lewis rats (Rat adjuvant-induced arthritis model)
Dosage:0.1, 0.3, 1, 3, 10 mg/kg
Administration:Oral gavage; twice a day for 10 days
Result:Inhibited disease pathology in rat adjuvant induced arthritis.
体外研究:
In biochemical assays, Upadacitinibis 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 Upadacitinibfor JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.