PF-5081090 (LpxC-4) is a potentLpxCinhibitor, is a rapidly bactericidal with broad-spectrum activity. PF-5081090 serves as a regulator of lipid A biosynthesis in Gram-negative pathogens^[1][2].

PF-5081090 shows strong potency against a broad spectrum of Gram-negative pathogens with IC₅₀s of 1.1 nM (P.aeruginosa), 0.069 nM (K.pneumonia) and MIC₉₀s of 1 μg/mL (P.aeruginosa,K.pneumoniae), 0.25 μg/mL (E.coli), 0.5 μg/mL (Enterobacterspp), 2 μg/mL (S.maltophilia)^[1].
PF-5081090 (0.25 μg/mL; 0-50 h) demonstrates sustained bactericidal activities againstP.aeruginosaUC12120 (A), PA-1955 (B), andK.pneumoniaeKP-1487^[1].
PF-5081090 (32 mg/L) increases antibiotic susceptibility in Acinetobacter baumannii with rifampicin, vancomycin, azithromycin, imipenem and amikacin^[2].
PF-5081090 (32 mg/L) inhibits lipid A biosynthesis, and significantly increases cell permeability inA.baumannii^[2].

PF-5081090 (8.75, 75, 300 mg/kg; s.c.; single dose) exhibits a exposure increasing in linear manner across the dose range in mice, with area under the concentration-time curve (AUC) and maximum concentration of drug in serum (C_max) increasing with a proportional increase in dose^[1].
PF-5081090 shows potent efficacies against sentinel strains ofP.aeruginosaandK.pneumoniain CD-1 mice, with effective dose (ED₅₀) ranging from 7.4-55.9 mg/kg (against acute septicemia model),<25 mgkg (against pneumonia model), and 16.8 neutropenicthigh model) in mice infected withP.aeruginosaPA-1950^[1].
Pharmacokinetics of PF-5081090 in CD-1 mice^a[1]

412.43

C₁₈H₂₁FN₂O₆S

1312473-63-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.