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首页-小分子抑制剂&激动剂-GPCR-Glucagon Receptor-AZD0186
AZD0186

Chemical Structure : AZD0186

CAS No.: 2922542-61-6

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AZD0186 (AZD-0186)

货号: PC-25613Not For Human Use, Lab Use Only.

AZD0186 (AZD-0186) is a potent, selective glucagon-like peptide-1 receptor (GLP-1R) agonist, shows concentration-dependent potentiation of GSIS in EndoC-βH5 cells with EC50 of 0.6 nM, improves glucose control and reduces body weight.

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

    生物&药学活性

    AZD0186 (AZD-0186) is a potent, selective glucagon-like peptide-1 receptor (GLP-1R) agonist, shows concentration-dependent potentiation of GSIS in EndoC-βH5 cells with EC50 of 0.6 nM, improves glucose control and reduces body weight.
    AZD0186 concentration dependently binds to the hGLP-1R displacing radiolabeled GLP-1(7–36)NH2 as well as potentiates cAMP accumulation in hGLP-1R overexpressing cells.
    AZD0186 is a partial agonist in the β-arrestin-2 assay and full agonist in GLP-1R internalization assay.
    AZD0186 exhibits a concentration-dependent effect on potentiating insulin secretion at 11 mM glucose in EndoC-βH5 cell line.
    AZD0186 improves glucose control and reduces body weight in a human glucagon-like peptide-1 receptor mouse model.

    物理化学性质&存储条件

    分子量 636.53
    分子式 C32H31Cl2N5O5
    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

    4-chloro-2-(((1R,6R)-5-((S)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)-2,5-diazabicyclo[4.2.0]octan-2-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid

    参考文献

    1. Weier Qi, et al. J Pharmacol Exp Ther. 2025 Aug 28;392(10):103683.

    2. Patent WO2023057427.

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