S82790 |
Upadacitinib |
| 源叶(MedMol) | 99% |
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- 产品描述： 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
- 靶点： JAK1:0.043 μM (IC50);JAK2:0.2 μM (IC50);JAK3:2.3 μM (IC50);Tyk2:4.7 μM (IC50)
- 体外研究： 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
- 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.
- 参考文献：
1. Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. 2. J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823. 3. Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494). BMC Rheumatol. 2018 Aug 28;2:23.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.629 ml 13.145 ml 26.29 ml 5 mM 0.526 ml 2.629 ml 5.258 ml 10 mM 0.263 ml 1.315 ml 2.629 ml 50 mM 0.053 ml 0.263 ml 0.526 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
