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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-ASP5736
ASP5736

Chemical Structure : ASP5736

CAS No.: 1264206-74-7

ASP5736 (ASP-5736)

货号: PC-49160Not For Human Use, Lab Use Only.

AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.

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

    生物&药学活性

    AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.
    AS5736 displays 30-fold greater selectivity for 5-HT5A over 5-HT7 receptor, and no significant affinity for 5-HT2A/2B/2C/3/4/6 receptors.
    AS5736 (0.001-0.003 mg/kg, p.o.) ameliorated scopolamine-induced working memory deficit in mice and improved reference memory impairment in aged rats.
    ASP5736 decreased the binding of LSD to 5-HT5A receptors in the olfactory bulb of rats in a dose-dependent manner and occupied 15%-50% of brain 5-HT5A receptors at behaviorally effective doses.

    物理化学性质&存储条件

    分子量 461.357
    分子式 C20H14F3N5O5
    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

    N-(diaminomethylene)-1-(3,5-difluoropyridin-4-yl)-4-fluoroisoquinoline-7-carboxamide fumarate

    参考文献

    1. Yamazaki M, et al. J Pharmacol Sci. 2015 Mar;127(3):362-9.

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