Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Upadacitinib tartrate
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1607431-21-9

1607431-21-9 structure

Name: Upadacitinib tartrate
Chemical Name: Upadacitinib tartrate
CAS Number: 1607431-21-9
Molecular Formula: C₂₁H₃₃F₃N₆O₁₁
Molecular Weight: 602.516
Catalog: Signaling Pathways Epigenetics JAK
Create Date: 2018-07-18 22:43:58
Modify Date: 2024-01-04 17:09:18
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].

Name	Upadacitinib tartrate
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

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	Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK Research Areas >> Inflammation/Immunology
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.

Molecular Formula	C₂₁H₃₃F₃N₆O₁₁
Molecular Weight	602.516
Exact Mass	602.215942

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