PF-04753299 是一种有效的选择性 UDP-3-O-(R-3-hydroxymyristol)-N-乙酰氨基葡萄糖脱乙酰酶 (LpxC) 抑制剂。
货号:ajcx26456
CAS:1289620-49-0
分子式:C18H21NO4S
分子量：347.4
溶解度:DMSO: 34.7mg/mL
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-04753299 is an inhibitor of LpxC (IC₅₀= 1.37 nM), a bacterial deacetylase involved in the biosynthesis of LPS lipid A.¹It is selective for LpxC over a panel of 16 human matrix metalloproteinases (MMPs; K_is = >1 µM for all). PF-04753299 is active againstP. aeruginosa, K. pneumoniae, E. coli, E. aerogenes, C. freundii, andA. 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 systemicP. aeruginosainfection (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)