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VB-82252

Chemical Structure : VB-82252

CAS No.: 2170004-34-7

VB-82252 (VB82252)

Catalog No.: PC-35006Not For Human Use, Lab Use Only.

VB-82252 is a highly potent, orally active inhibitor of C. difficile toxins TcdA and TcdB, potently inhibits UDP glucose hydrolysis activity of TcdB (IC50=32 nM).

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    Biological Activity

    VB-82252 is a highly potent, orally active inhibitor of C. difficile toxins TcdA and TcdB, potently inhibits UDP glucose hydrolysis activity of TcdB (IC50=32 nM).
    VB-82252 protects CHO-K1 cells against challenge with purified TcdA (IC50 = 5.0 uM) or TcdB (IC50=0.25 uM).
    VB-82252 prevents inflammation in murine intrarectal toxin challenge model, reduces weight loss and gut inflammation during acute disease in murine model of recurrent Clostridium difficile infection (CDI), demonstrates efficacy similar to that of vancomycin.

    Physicochemical Properties

    M.Wt 614.406
    Formula C29H20Cl2F3N5O3
    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)-2-chloro-4-((8-chloro-2,5-dioxo-3-(pyridin-2-ylmethyl)-1,2,3,5-tetrahydro-4H-benzo[e][1,4]diazepin-4-yl)methyl)-N-(5-(trifluoromethyl)pyridin-2-yl)benzamide

    References

    1. Stroke IL, et al. Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: e00107-18.

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