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首页-小分子抑制剂&激动剂-GPCR-mAChR-AZD8871
AZD8871

Chemical Structure : AZD8871

CAS No.: 1435519-06-4

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AZD8871 (AZD-8871, Navafenterol)

货号: PC-72979Not For Human Use, Lab Use Only.

AZD8871 (AZD-8871, Navafenterol) is a potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with pIC50 9.5 for human M3 receptor, pEC50 9.5 for β2-adrenoceptor.

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

    生物&药学活性

    AZD8871 (AZD-8871, Navafenterol) is a potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with pIC50 9.5 for human M3 receptor, pEC50 9.5 for β2-adrenoceptor.
    AZD8871 is selective for the β2-adrenoceptor over the β1 and β3 subtypes (3- and 6-fold, respectively) and shows dual antimuscarinic and β2-adrenoceptor functional activity in isolated guinea pig tissue (pIC50=8.6).
    AZD8871 exhibits a higher muscarinic component than batefenterol in human bronchi, with a shift in potency under propranolol blockade of 2- and 6-fold, respectively.
    AZD8871 prevents acetylcholine-induced bronchoconstriction in both guinea pig and dog with minimal effects on salivation and heart rate at doses with bronchoprotective activity.

    物理化学性质&存储条件

    分子量 742.91
    分子式 C38H42N6O6S2
    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

    trans-4-[[3-[5-[[[(2R)-2-(1,2-Dihydro-8-hydroxy-2-oxo-5-quinolinyl)-2-hydroxyethyl]amino]methyl]-1H-benzotriazol-1-yl]propyl]methylamino]cyclohexyl α-hydroxy-α-2-thienyl-2-thiopheneacetate

    参考文献

    1. Singh D, et al. Respir Res. 2020 Sep 9;21(Suppl 1):102.

    2. Balaguer V, et al. Respir Res. 2020 Sep 9;21(Suppl 1):212.

    3. Aparici M, et al. J Pharmacol Exp Ther. 2019 Jul;370(1):127-136.

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