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Upadacitinib tartrate tetrahydrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Upadacitinib tartrate tetrahydrate图片
CAS NO:1607431-21-9
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ABT-494 tartrate tetrahydrate
产品介绍
Upadacitinib (ABT-494) tartrate tetrahydrate 是一种高效的、具有口服活性的、选择性 Janus 激酶 1 (JAK1) 抑制剂 (IC50=43 nM)。Upadacitinib tartrate tetrahydrate 对 JAK1 的选择性约为 JAK2 (200 nM）的 74 倍。Upadacitinib tartrate tetrahydrate 可用于多种自身免疫性疾病的研究。
生物活性

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 forJAK1overJAK2(200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research[1][2].

IC50& Target[1]

JAK1

0.043 μM (IC50)

JAK2

0.2 μM (IC50)

JAK3

2.3 μM (IC50)

Tyk2

4.7 μM (IC50)

体外研究
(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].

体内研究
(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.
Clinical Trial
分子量

602.52

Formula

C17H19F3N6O.C4H6O6.4H2O

CAS 号

1607431-21-9

中文名称

乌帕替尼四水酒石酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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