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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-TP455
TP455

Chemical Structure : TP455

CAS No.: 2042563-95-9

TP455 (TP-455;TP 455)

货号: PC-35297Not For Human Use, Lab Use Only.

TP455 (TP-455) is a highly potent, selective A2A adenosine receptor inverse agonist with IC50 of 1.9 nM in cyclic AMP assays in hA2A CHO cells.

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

    生物&药学活性

    TP455 (TP-455) is a highly potent, selective A2A adenosine receptor inverse agonist with IC50 of 1.9 nM in cyclic AMP assays in hA2A CHO cells.
    TP455 proved to be more potent than morphine in writhing and tail immersion tests in mice with ED50 of 0.0328 mg/kg, exhibits great analgesic activity with an ED50 of 0.134 ± 0.011 mg/kg and minimum effective dose of 0.01 mg/kg.
    TP455 antagonizes CGS 21680-induced cell proliferation in cancer cell lines, inhibits GS 21680-dependent pERK1/2, pJNK MAPK kinase, and pAKT activation.

    物理化学性质&存储条件

    分子量 353.4
    分子式 C17H15N5O2S
    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

    2-(2-furanyl)-N5-(2-methoxybenzyl)[1,3]thiazolo[5,4-d]pyrimidine-5,7-diammine

    参考文献

    1. Gessi S, et al. Front Pharmacol. 2017 Dec 1;8:888. doi: 10.3389/fphar.2017.00888.

    2. Varano F, et al. J Med Chem. 2016 Dec 8;59(23):10564-10576.

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