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首页-小分子抑制剂&激动剂-GPCR-Opioid Receptor-PF-04455242 hydrochloride
PF-04455242 hydrochloride

Chemical Structure : PF-04455242 hydrochloride

CAS No.: 1322001-35-3

PF-04455242 hydrochloride (PF-4455242)

货号: PC-62109Not For Human Use, Lab Use Only.

PF-04455242 hydrochloride is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.

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

    生物&药学活性

    PF-04455242 hydrochloride is a potent, selective κ-opioid receptor (KOR) antagonist with Ki of 3 nM/21 nM/22 nM for hKOR/rKOR/mKOR, respectively.
    PF-04455242 shows 20-fold reduced affinity for hMOR and negligible affinity for DOR (Ki>4 uM).
    PF-04455242 demonstrates antidepressant-like efficacy, attenuates the behavioral effects of stress, dose-dependently reduceds the elevation of spiradoline-induced plasma prolactin in rats.

    物理化学性质&存储条件

    分子量 408.985
    分子式 C21H29ClN2O2S
    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

    2-Methyl-N-[[4-(2-pyrrolidin-1-ylsulfonylphenyl)phenyl]methyl]propan-1-amine hydrochloride

    参考文献

    1. Verhoest PR, et al. J Med Chem. 2011 Aug 25;54(16):5868-77.

    2. Grimwood S, et al. J Pharmacol Exp Ther. 2011 Nov;339(2):555-66.

    3. Melief EJ, et al. Mol Pharmacol. 2011 Nov;80(5):920-9.

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