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首页-小分子抑制剂&激动剂-GPCR-mAChR-PF-06764427
PF-06764427

Chemical Structure : PF-06764427

CAS No.: 1842371-08-7

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PF-06764427 (PF06764427)

货号: PC-35477Not For Human Use, Lab Use Only.

PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors 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-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM.
    PF-06764427 induces a 212-fold shift in the ACh CRC at 10 uM in the PathHunter Arrβ2 assay.
    PF-06764427 demonstrates robust potentiation of acetylcholine across the G-protein and Arrβ2 pathways, adequate brain availability, favorable pharmacokinetic properties and invivo efficacy in a mouse amphetamine-stimulated LMA model.

    物理化学性质&存储条件

    分子量 431.496
    分子式 C24H25N5O3
    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

    1-[4-(1-Methyl-1H-pyrazol-3-yl)-benzyl]-1H-pyrrolo[3,2-b]pyridine-3-carboxylic acid (3R,4S)-(3-hydroxy-tetrahydro-pyran-4-yl)-amide

    参考文献

    1. Moran SP, et al. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771.

    2. Rook JM, et al. ACS Chem Neurosci. 2018 May 8. doi: 10.1021/acschemneuro.8b00131.

    3. Davoren JE, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655.

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