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Xeruborbactam

Chemical Structure : Xeruborbactam

CAS No.: 2170834-63-4

Xeruborbactam (QPX7728)

Catalog No.: PC-73346Not For Human Use, Lab Use Only.

Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor, inhibits class A extended-spectrum beta-lactamases with IC50 of 1-3 nM, carbapenemases such as KPC (IC50, 2.9 nM), class C P99 (IC50, 22 nM).

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    Biological Activity

    Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor, inhibits class A extended-spectrum beta-lactamases with IC50 of 1-3 nM, carbapenemases such as KPC (IC50, 2.9 nM), class C P99 (IC50, 22 nM).
    QPX7728 displays a remarkably broad spectrum of inhibition, including class B and class D enzymes.
    QPX7728 is also a potent inhibitor of class D carbapenemases such as OXA-48 from Enterobacteriaceae and OXA enzymes from Acinetobacter baumannii (OXA-23/24/58, IC50 range, 1 to 2 nM) as well as MBLs such as NDM-1 (IC50, 55 ± 25 nM), VIM-1 (IC50, 14 ± 4 nM), and IMP-1 (IC50, 610 ± 70 nM).
    QPX7728 restored the potency of meropenem against carbapenem-resistant Enterobacterales (CRE), with the meropenem MIC90 decreasing from >64 μg/ml to 0.5 μg/ml for QPX7728 (8 μg/ml).

    Physicochemical Properties

    M.Wt 221.98
    Formula C10H8BFO4
    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

    (1aR,7bS)-5-Fluoro-1,1a,2,7b-tetrahydro-2-hydroxybenzo[e]cycloprop[c][1,2]oxaborin-4-carboxylic acid

    References

    1. Hecker SJ, et al. J Med Chem. 2020 Jul 23;63(14):7491-7507.

    2. Lomovskaya O, et al. Front Microbiol. 2021 Jul 5;12:697180.

    3. Lomovskaya O, et al. Antimicrob Agents Chemother. 2021 May 18;65(6):e00210-21.

    4. Nelson K, et al. Antimicrob Agents Chemother. 2020 Oct 20;64(11):e01406-20.

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