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DSP-0509

Chemical Structure : DSP-0509

CAS No.: 1488364-57-3

DSP-0509 (DSP0509, Guretolimod)

Catalog No.: PC-21818Not For Human Use, Lab Use Only.

DSP-0509 (DSP0509) is a potent selective small-molecule TLR7 agonist with EC50 of 515 nM and 33 nM in cells expressing human and murine TLR7, respectively.

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    Biological Activity

    DSP-0509 (Guretolimod) is a potent selective small-molecule TLR7 agonist with EC50 of 515 nM and 33 nM in cells expressing human and murine TLR7, respectively.
    DSP-0509 displays no agonistic activity against TLR8 up to 100 uM.
    DSP-0509 (1 uM) induced the secretion of cytokines including type-I interferons and the elevation of MHC class II expression in bone marrow-derived dendritic cells (BMDCs) differentiated from murine bone marrow cells.
    DSP-0509 induced IFNα dose dependent manner in human primary pDC.
    DSP-0509 (5 mg/kg i.v.) exhibited T cell-dependent anti-tumor effects in CT26 models.
    DSP-0509 in combination with anti-PD-1 antibody, anti-CTLA-4 antibody additively enhanced anti-tumor activity.

    Physicochemical Properties

    M.Wt 513.56
    Formula C24H34F3N5O4
    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

    (S)-N-(4-((2-amino-4-((1-hydroxyhexan-3-yl)amino)-6-methylpyrimidin-5-yl)methyl)-3-methoxybenzyl)-N-(2,2,2-trifluoroethyl)glycine

    References

    1. Ota Y, et al. Front Immunol. 2023 Jan 30;14:1055671.

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