Upadacitinib

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Chemical Structure| 1310726-60-3 同义名 : ABT-494
CAS号 : 1310726-60-3
货号 : A165008
分子式 : C17H19F3N6O
纯度 : 99%+
分子量 : 380.37
MDL号 : MFCD30502663
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(276.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Upadacitinib (ABT-494) emerges as a highly potent, orally administered, JAK1-selective inhibitor, boasting an IC50 value of 43 nM. It displays roughly 74 times more affinity for JAK1 over JAK2 (200 nM) in cell-based assays that hinge on particular, pertinent cytokines, making it a viable option for researching various autoimmune diseases[1].[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.15mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL
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.