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TP455

Chemical Structure : TP455

CAS No.: 2042563-95-9

TP455 (TP-455;TP 455)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 353.4
    Formula C17H15N5O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

    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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