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Tyk2-IN-4(BMS-986165)
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。
Tyk2-IN-4(BMS-986165)图片
CAS NO:1609392-27-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Tyk2-IN-4 (BMS-986165) (BMS-986165) 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂,用于治疗自身免疫性疾病,选择性结合 TYK2 假激酶 (JH2) 结构域 (IC50=1.0 nM) 并阻断受体介导的 Tyk2 激活通过稳定调节 JH2 结构域。
Cas No.1609392-27-9
别名BMS-986165
Canonical SMILESO=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]
分子式C20H19D3N8O3
分子量425.46
溶解度DMSO : 62.5 mg/mL (146.90 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).

Tyk2-IN-4 blocks receptor-mediated Tyk2 activation by stabilizing the regulatory pseudokinase domain of the protein[1].

Lupus-like disease is strongly inhibited in NZB/W mice treated with Tyk2-IN-4. Tyk2-IN-4 is safe and overall well-tolerated. There are no serious adverse events and the frequency of non-serious adverse events are similar in the active (75%) and placebo (76%) groups. After oral administration, Tyk2-IN-4 is rapidly absorbed and exhibits an apparent elimination half-life of 8-15 hours[1].

[1]. I Catlett, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2.