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SX-517

Chemical Structure : SX-517

CAS No.: 1240494-13-6

SX-517 (Phenylboronic Acid;SX 517;SX517)

Catalog No.: PC-60620Not For Human Use, Lab Use Only.

SX-517 is a potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.

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    Biological Activity

    SX-517 is a potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.
    SX-517 inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2.
    SX-517significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).

    Physicochemical Properties

    M.Wt 382.216
    Formula C19H16BFN2O3S
    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-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid

    References

    1. Maeda DY, et al. J Med Chem. 2014 Oct 23;57(20):8378-97.

    2. Schuler AD, et al. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3793-7.

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