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Upadacitinib tartrate tetrahydrate

CAS: 1607431-21-9 F: C17H19F3N6O.C4H6O6.4H2O W: 602.52

Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (I
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Bioactivity Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].
Invitro In biochemical assays, Upadacitinib tartrate tetrahydrate 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)[1].
In Vivo Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) tartrate tetrahydrate demonstrates efficacy in rat arthritis models[3]. Animal Model:
Name Upadacitinib tartrate tetrahydrate
CAS 1607431-21-9
Formula C17H19F3N6O.C4H6O6.4H2O
Molar Mass 602.52
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [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.