An inhibitor of LpxC
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PF-04753299

Item No. 36502

Technical Information
Formal Name
N-hydroxy-αR-methyl-α-(methylsulfonyl)-[1,1′-biphenyl]-4-butanamide
CAS Number
1289620-49-0
Molecular Formula
C18H21NO4S
Formula Weight
Purity
≥98%
A solid
DMSO: 34.7mg/mL
SMILES
ONC([C@@](S(C)(=O)=O)(C)CCC1=CC=C(C2=CC=CC=C2)C=C1)=O
InChi Code
InChI=1S/C18H21NO4S/c1-18(17(20)19-21,24(2,22)23)13-12-14-8-10-16(11-9-14)15-6-4-3-5-7-15/h3-11,21H,12-13H2,1-2H3,(H,19,20)/t18-/m1/s1
InChi Key
GDYIQUFNICPYHF-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brown, M.F., Reilly, U., Abramite, J.A., et alPotent inhibitors of LpxC for the treatment of Gram-negative infections. J. Med. Chem. 55(2), 914-923 (2012).