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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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Purity & Documentation Purity: >98% (HPLC)

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); protects CHO-K1 cells against challenge with purified TcdA (IC50 = 5.0 uM) or TcdB (IC50=0.25 uM); 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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