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CXCR2 inhibitor 68

Chemical Structure : CXCR2 inhibitor 68

CAS No.: 1838123-21-9

CXCR2 inhibitor 68 (CXCR2-IN-2)

Catalog No.: PC-62775Not For Human Use, Lab Use Only.

CXCR2-IN-68 is a potent, selective, brain penetrant, and orally bioavailable CXCR2 antagonist with pIC50 of 9.0, displays 730-fold selectivity over CXCR1 and >1,900-fold selectivity over all other chemokine receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    CXCR2 inhibitor 68 is a potent, selective, brain penetrant, and orally bioavailable CXCR2 antagonist with pIC50 of 9.0, displays 730-fold selectivity over CXCR1 and >1,900-fold selectivity over all other chemokine receptors.
    CXCR2 inhibitor 68 inhibits human whole blood Gro-α induced CD11b expression with IC50 of 0.04 µM, 17-fold more potent than Navarixin.
    CXCR2 inhibitor 68 significantly inhibits neutrophil infiltration in mouse at 1, 3, 10 mg/kg oral dosing twice daily (BID).

    Physicochemical Properties

    M.Wt 414.901
    Formula C18H23ClN2O5S
    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

    1-(4-chloro-2-hydroxy-3-(((S)-3-methyltetrahydrofuran-3-yl)sulfonyl)phenyl)-3-((R)-2-methylcyclopent-2-en-1-yl)urea

    References

    1. Lu H, et al. J Med Chem. 2018 Feb 28. doi: 10.1021/acs.jmedchem.7b01854.

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