PF-04753299 是一种有效的、选择性的LpxC抑制剂。PF-04753299 对淋球菌分离株具有杀菌作用，对大肠杆菌、铜绿假单胞菌和肺炎菌株的抑制的MIC90值分别为 2 μg/ml、4 μg/ml 和 16 μg/ml。PF-04753299 用于革兰氏阴性菌感染的研究。

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC). PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC 90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection [1].

Mice were administered PF-04753299 (subcutaneous dose; vehicle: 40% β cyclodextrin in water) 0.5 and 4 h after an intraperitoneal challenge of Pseudomonas aeruginosa strain UC12120, a penicillin-resistant, quinolone-sensitive clinical isolate (1a MIC = 0.25 μg/mL). At 24 h postinfection, the animals were sacrificed and the bacterial burden in the spleen was determined. The drug dose providing 50% bacterial burden reduction relative to untreated animals (ED50) was determined to be 35 mg/kg[2].

1289620-49-0

C18H21NO4S

347.43

PF-04753299

DMSO:18mg/mL (51.8mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years