Upadacitinib tartrate

Modify Date: 2024-01-04 17:09:18

Upadacitinib tartrate Structure
Upadacitinib tartrate structure
Common Name Upadacitinib tartrate
CAS Number 1607431-21-9 Molecular Weight 602.516
Density N/A Boiling Point N/A
Molecular Formula C21H33F3N6O11 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Upadacitinib tartrate


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].

 Names

Name Upadacitinib tartrate
Synonym More Synonyms

 Upadacitinib tartrate Biological Activity

Description 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].
Related Catalog
Target

JAK1:0.043 μM (IC50)

JAK2:0.2 μM (IC50)

JAK3:2.3 μM (IC50)

Tyk2:4.7 μM (IC50)

In Vitro 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: Female Lewis rats (Rat adjuvant-induced arthritis model)[3] 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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C21H33F3N6O11
Molecular Weight 602.516
Exact Mass 602.215942

 Synonyms

Upadacitinib tartrate
(3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide (2R,3R)-2,3-dihydroxybutanedioate, tetrahydrate
(2R,3R)-2,3-Dihydroxysuccinic acid - (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide hydrate (1:1:4)
Butanedioic acid, 2,3-dihydroxy-, (2R,3R)-, compd. with (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide, hydrate (1:1:4)
ABT-494
UNII-7KCW9IQM02