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ChemR23 inhibitor 14f

Chemical Structure : ChemR23 inhibitor 14f

CAS No.: 3032433-98-7

ChemR23 inhibitor 14f

Catalog No.: PC-72833Not For Human Use, Lab Use Only.

ChemR23 inhibitor 14f is a potent and orally active inhibitor of ChemR23 (IC80=12 nM), a G protein-coupled receptor (GPCR) expressed on the surface of plasmacytoid dendritic cells (pDCs).

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    Biological Activity

    ChemR23 inhibitor 14f is a potent and orally active inhibitor of ChemR23 (IC80=12 nM), a G protein-coupled receptor (GPCR) expressed on the surface of plasmacytoid dendritic cells (pDCs).
    ChemR23 inhibitor 14f inhibits ChemR23 signaling through receptor internalization.
    Oral administration of ChemR23 inhibitor 14f at 30 mg/kg to cynomolgus monkeys demonstrated a sustained pharmacological effect of ChemR23 internalization on pDCs.

    Physicochemical Properties

    M.Wt 619.755
    Formula C31H33N5O5S2
    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

    (R)-5-cyclopropyl-2-((cyclopropylmethyl)(1-(5'-methyl-2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)ethyl)amino)-N-(cyclopropylsulfonyl)thiazole-4-carboxamide

    References

    1. Takamichi Imaizumi, et al. Bioorg Med Chem. 2022 Feb 15;56:116587.

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