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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-CPL409116
CPL409116

Chemical Structure : CPL409116

CAS No.: 2250013-34-2

CPL409116 (CPL 409116)

货号: PC-49651Not For Human Use, Lab Use Only.

CPL409116 (CPL 409116) is a potent, competitive, dual JAK and ROCK inhibitor with IC50 of 0.95/5.36//0.87/110.6/106.7 nM for JAK1/JAK2/JAK3/ROCK1/ROCK2, respectively.

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

    生物&药学活性

    CPL409116 (CPL 409116) is a potent, competitive, dual JAK and ROCK inhibitor with IC50 of 0.95/5.36//0.87/110.6/106.7 nM for JAK1/JAK2/JAK3/ROCK1/ROCK2, respectively.
    CPL409116 is a selective JAK/ROCK inhibitor, and is more specific towards JAK1 and JAK3 than JAK2.
    CPL409116 blocked phosphorylation of JAK and ROCK kinase substrates STAT and MYPT, respectively.
    CPL409116 efficiently blocked expression of a broad range of cytokines, efficiently blocked CD4 T cell proliferation with IC50 of 59 nM.
    CPL409116 (40 mg/kg QD) improved survival and clinical parameters of murine lupus, ameliorated kidney nephropathy.

    物理化学性质&存储条件

    分子量 498.55
    分子式 C25H26N10O2
    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

    (R)-7-((1-(6-cyanopyridazin-3-yl)-3,3-dimethylpiperidin-4-yl)amino)-2-(6-methoxypyridin-2-yl)pyrazolo [1,5-a]pyrimidine-6-carboxamide

    参考文献

    1. Dulak-Lis M, et al. J Pharmacol Sci. 2021 Apr;145(4):340-348.

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