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TLR7-TLR8 agonist 31

Chemical Structure : TLR7-TLR8 agonist 31

CAS No.: 1413944-59-8

TLR7-TLR8 agonist 31

Catalog No.: PC-35315Not For Human Use, Lab Use Only.

TLR7 and 8 modulator 31 is a potent, orally active, dual TLR7 and 8 agonist with LEC values of 0.15 and 0.16 uM, respectively.

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    Biological Activity

    TLR7/TLR8 modulator 31 is a potent, orally active, dual TLR7 and 8 agonist with LEC values of 0.15 and 0.16 uM, respectively.
    TLR7/TLR8 modulator 31 displays a good off-target profile (Aa1A, D1, 5HT2A IC50>10 µM; CYP 2D6 IC50=5.7 µM), also shows no significant activity against a panel of 80 receptors.
    TLR7/TLR8 modulator 31 induces IFNα and pro-inflammatory cytokines at low dose in vivo, inhibits HBV replication indirectly, via cytokine induction and immune cells activation.
    TLR7/TLR8 modulator 31 induces endogenous IFNα, an interferon stimulated gene response (ISGs), and also activation of myeloid dendritic cells and monocytes towards a TH1 phenotype in both mice and cynomolgus monkeys in vivo.

    Physicochemical Properties

    M.Wt 278.331
    Formula C14H19FN4O
    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)-3-((2-Amino-8-fluoroquinazolin-4-yl)amino)hexan-1-ol

    References

    1. Embrechts W, et al. J Med Chem. 2018 Jul 2. doi: 10.1021/acs.jmedchem.8b00643.

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