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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-nAChR-TC-6683
TC-6683

Chemical Structure : TC-6683

CAS No.: 1025007-04-8

TC-6683 (AZD1446, AZD-1446, TC6683)

货号: PC-72282Not For Human Use, Lab Use Only.

TC-6683 (AZD1446) is a potent and highly selective α4β2 nAChR agonist with Ki of 30/34 nM against hα4β2/rα4β2, with little to no affinity against h α3β2 and h α7 (Ki>6.7 uM).

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

    生物&药学活性

    TC-6683 (AZD1446) is a potent and highly selective α4β2 nAChR agonist with Ki of 30/34 nM against hα4β2/rα4β2, with little to no affinity against h α3β2 and h α7 (Ki>6.7 uM).
    TC-6683 (10 uM) produced <30% inhibition of specific binding or enzyme activity at all targets except the human (87%) and murine (97%) 5-HT3 receptors at a panel of 70 receptors, ion channels, and enzymes at NovaScreen/Caliper.
    TC-6683 (AZD1446) enhanced working memory in the object recognition paradigm in rats at every dose tested (0.1−3 mg/kg, po), exhibited favorable pharmaceutical properties and in vivo efficacy in animal models.

    物理化学性质&存储条件

    分子量 240.687
    分子式 C11H13ClN2O2
    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

    (5-chlorofuran-2-yl)(hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)methanone

    参考文献

    1. Mazurov AA, et al. J Med Chem. 2012 Nov 8;55(21):9181-94.

    2. Jucaite A, et al. Psychopharmacology (Berl). 2014 Mar;231(6):1251-65.

    3. Canning BJ, et al. J Pharmacol Exp Ther. 2022 Feb;380(2):94-103.

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