Upadacitinib (tartraattetrahydraat)

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].

1607431-21-9

ABT-494 (tartrate tetrahydrate)

12352005

H302-H312-H332

JAK

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

COVID-19-immunoregulation

Inflammation/Immunology

10 mM in DMSO

O=C(NCC(F)(F)F)N1C[C@H]([C@H](C1)C2=CN=C3C=NC4=C(N32)C=CN4)CC.O=C([C@@H]([C@H](C(O)=O)O)O)O.[4.H2O]

C17H19F3N6O.C4H6O6.4H2O

602.52

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P363-P501

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-19569A/

Reference compound1

Launched

JAK1; JAK2; JAK3; Tyk2