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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Ropsacitinib
Ropsacitinib

Chemical Structure : Ropsacitinib

CAS No.: 2127109-84-4

Ropsacitinib (PF-06826647)

货号: PC-72613Not For Human Use, Lab Use Only.

Ropsacitinib (PF-06826647) is a potent, selective TYK2 inhibitor with IC50 of 15 nM, inhibits JAK1/2/3 with IC50 of 383/74/>10,000 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ropsacitinib (PF-06826647) is a potent, selective TYK2 inhibitor with IC50 of 15 nM, inhibits JAK1/2/3 with IC50 of 383/74/>10,000 nM.
Ropsacitinib (PF-06826647) targets and binds to the JH1 domain, inhibits IL-12 stimulated phosphorylation of STAT4 with IC50 of 14 nM.
Ropsacitinib (PF-06826647) (1-30 mg/kg, po, QD) inhibits ear swelling in the imiquimod-induced skin inflammation model.

物理化学性质&存储条件

分子量 383.419
分子式 C20H17N9
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 (3.8 mg/mL)

Chemical Name/SMILES

(1r,3r)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile

参考文献

1. Gerstenberger BS, et al. J Med Chem. 2020 Nov 25;63(22):13561-13577.

2. Singh RSP, et al. Clin Transl Sci. 2021 Mar;14(2):671-682.

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