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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-AQW-051
AQW-051

Chemical Structure : AQW-051

CAS No.: 669770-29-0

AQW-051 (AQW051;AQW 051)

货号: PC-61600Not For Human Use, Lab Use Only.

AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56.

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

    生物&药学活性

    AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56; displays high selectivity (>100-fold) over other nACh receptors; stimulates calcium influx in GH3–ha7-22 cells recombinantly expressing the human α7-nACh receptor with pEC50 of 7.41; facilitates learning/memory performance in mice; reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys.

    Parkinson Disease

    Phase 2 Clinical

    物理化学性质&存储条件

    分子量 294.398
    分子式 C19H22N2O
    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

    (3R)-3-{[6-(4-methylphenyl)pyridin-3-yl]oxy}-1-azabicyclo[2.2.2]octane

    参考文献

    1. Feuerbach D, et al. Br J Pharmacol. 2015 Mar;172(5):1292-304.

    2. Di Paolo T, et al. Parkinsonism Relat Disord. 2014 Nov;20(11):1119-23.

    3. Beinat C, et al. CNS Drugs. 2015 Jul;29(7):529-42.

    4. Trenkwalder C, et al. Mov Disord. 2016 Jul;31(7):1049-54.

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