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首页-小分子抑制剂&激动剂-GPCR-mAChR-PF-06827443
PF-06827443

Chemical Structure : PF-06827443

CAS No.: 2115022-67-6

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PF-06827443 (PF06827443)

货号: PC-35482Not For Human Use, Lab Use Only.

PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM.

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

    生物&药学活性

    PF-06827443 (PF06827443) is a potent, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with EC50 of 47 nM, shows no activity against M2-M5 at 10 uM.
    PF-06827443 induces cholinergic adverse events and convulsion at therapeutic indices similar to previous compounds with more agonist activity.

    物理化学性质&存储条件

    分子量 404.466
    分子式 C24H24N2O4
    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-((3R,4S)-3-Hydroxytetrahydro-pyran-4-yl)-5-methyl-6-(4-oxazol-4-yl-benzyl)-2,3-dihydro-isoindol-1-one

    参考文献

    1. Davoren JE, et al. J Med Chem. 2017 Aug 10;60(15):6649-6663.

    2. Moran SP, et al. ACS Chem Neurosci. 2018 Apr 25. doi: 10.1021/acschemneuro.8b00106.

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