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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-JNJ 41876666
JNJ 41876666

Chemical Structure : JNJ 41876666

CAS No.: 1259026-14-6

JNJ 41876666 (JNJ-41876666;JNJ41876666)

货号: PC-60719Not For Human Use, Lab Use Only.

JNJ 41876666 (JNJ-41876666) is a potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM.

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

    生物&药学活性

    JNJ 41876666 (JNJ-41876666) is a potent, selective, orally active TRPM8 channel antaognist with IC50 of 0.8 nM.
    JNJ 41876666 exhibits minimal effect on the enzyme activity of CYP isoforms 3A4, 1A2, 2D6, 2C9, and 2C19 (IC50>10 uM).
    JNJ 41876666 completely prevents icilin-induced WDS at an oral dose of 10 mg/kg, exhibits potent in vitro functional activity and robust oral efficacy in an inflammatory model of neuropathic pain at relatively low plasma levels.
    JNJ 41876666 also reduces proliferation rates and proliferative fraction in prostate cancer cells.

    物理化学性质&存储条件

    分子量 503.873
    分子式 C23H20ClF6N3O
    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

    3-[7-Trifluoromethyl-5-(2-trifluoromethyl-phenyl)-1H-benzimidazol-2-yl]-1-oxa-2-aza-spiro[4.5]dec-2-ene hydrochloride

    参考文献

    1. Valero ML, et al. PLoS One. 2012;7(12):e51825.

    2. Parks DJ, et al. J Med Chem. 2011 Jan 13;54(1):233-47.

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