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PF-5081090
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PF-5081090
CAS No. : 1312473-63-4
MCE 站:PF-5081090
产品活性:PF-5081090 (LpxC-4) 是一种强效的 LpxC 抑制剂,具有广谱、快速的杀菌活性。PF-5081090 能够调节革兰氏阴性菌中脂类 A 生物合成。
研究领域:Anti-infection
作用靶点:Antibiotic | Bacterial
In Vitro: 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 (Enterobacter spp), 2 μg/mL (S. maltophilia).
PF-5081090 (0.25 μg/mL; 0-50 h) demonstrates sustained bactericidal activities against P. aeruginosa UC12120 (A), PA-1955 (B), and K. pneumoniae KP-1487.
PF-5081090 (32 mg/L) increases antibiotic susceptibility in Acinetobacter baumannii with rifampicin, vancomycin, azithromycin, imipenem and amikacin.
PF-5081090 (32 mg/L) inhibits lipid A biosynthesis, and significantly increases cell permeability in A. baumannii.
In Vivo: 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 (Cmax) increasing with a proportional increase in dose.
PF-5081090 shows potent efficacies against sentinel strains of P. aeruginosa and K. pneumonia in CD-1 mice, with effective dose (ED50) ranging from 7.4-55.9 mg/kg (against acute septicemia model), <25 mg/kg (against pneumonia model), and 16.8 mg/kg (against neutropenic thigh model) in mice infected with P. aeruginosa PA-1950.
Pharmacokinetics of PF-5081090 in CD-1 micea
Dose (mg/kg) | Cmax (mg/L) | Tmax (h) | AUC (hmg/L) | Free AUC (hmg/L) | T1/2 (h) | CL (L/h/kg) | Vss (L/kg) |
18.75 | 5.02 | 0.25 | 5.09 | 1.58 | 0.6 | 3.79 | 2.20 |
75 | 15.50 | 0.33 | 17.60 | 5.46 | 0.69 | 4.32 | 3.30 |
300 | 75.40 | 0.33 | 76.30 | 23.70 | 0.68 | 3.92 | 2.53 |
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