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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-ESK-001 hydrochloride
ESK-001 hydrochloride

Chemical Structure : ESK-001 hydrochloride

CAS No.: 3009133-87-0

ESK-001 hydrochloride (Envudeucitinib hydrochloride)

货号: PC-25063Not For Human Use, Lab Use Only.

ESK-001 hydrochloride (Envudeucitinib) is a novel allosteric, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 104-149 nM in human whole blood, binds to JH2 domain of TYK2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ESK-001 hydrochloride (Envudeucitinib) is a novel allosteric, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 104-149 nM in human whole blood, binds to JH2 domain of TYK2.
ESK-001 (Envudeucitinib) has no off‐target effects on other kinases (IC50 of >30,000 nM for JAK1‐3).
ESK-001 (Envudeucitinib) significantly inhibited STAT phosphorylation and downstream IFNγ production stimulated by IL‐12, IL‐23, and IFNα in human whole blood and peripheral blood mononuclear cells in a concentration‐dependent manner.

物理化学性质&存储条件

分子量 462.97
分子式 C22H19D6ClN6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-((2-methoxy-3-(1-(methyl-d3)-1H-1,2,4-triazol-3-yl)phenyl)amino)-5-(propanoyl-3,3,3-d3)pyridin-2-yl)cyclopropanecarboxamide hydrochloride

参考文献

1. Ucpinar S, et al. Clin Transl Sci. 2024 Dec;17(12):e70094.

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