PF-04753299 |
| رقم الكتالوجGC49765 |
PF-04753299 هو مثبط قوي وانتقائي UDP-3-O- (R-3-hydroxymyristol) -N-acetylglucosamine deacetylase (LpxC)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1289620-49-0
Sample solution is provided at 25 µL, 10mM.
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PF-04753299 is an inhibitor of LpxC (IC50 = 1.37 nM), a bacterial deacetylase involved in the biosynthesis of LPS lipid A.1 It is selective for LpxC over a panel of 16 human matrix metalloproteinases (MMPs; Kis = >1 µM for all). PF-04753299 is active against P. aeruginosa, K. pneumoniae, E. coli, E. aerogenes, C. freundii, and A. baumannii (MIC90s = 4, 16, 2, 4, 8, and 32 µg/ml, respectively). In vivo, PF-04753299 reduces splenic bacterial burden in a mouse model of systemic P. aeruginosa infection (ED50 = 35 mg/kg).
1.Brown, M.F., Reilly, U., Abramite, J.A., et al.Potent inhibitors of LpxC for the treatment of Gram-negative infectionsJ. Med. Chem.55(2)914-923(2012)
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