For research use only. Not for therapeutic Use.
PF-5081090 (LpxC-4) is a potent LpxC inhibitor, 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 (Enterobacter spp), 2 μg/mL (S. maltophilia)[1].
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[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 in A. 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 (Cmax) increasing with a proportional increase in dose[1].
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[1].
Pharmacokinetics of PF-5081090 in CD-1 micea[1]
Dose (mg/kg)
Cmax (mg/L)
Tmax (h)
AUC (h•mg/L)
Free AUC (h•mg/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
a Following single subcutaneous doses.
| Catalog Number | R056247 |
| CAS Number | 1312473-63-4 |
| Synonyms | (2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1-yl]-N-hydroxy-2-methyl-2-methylsulfonylbutanamide |
| Molecular Formula | C18H21FN2O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C18H21FN2O6S/c1-18(17(23)20-24,28(3,25)26)7-9-21-8-6-12(10-16(21)22)14-5-4-13(27-2)11-15(14)19/h4-6,8,10-11,24H,7,9H2,1-3H3,(H,20,23)/t18-/m1/s1 |
| InChIKey | DNVUWHWBCMGQLU-GOSISDBHSA-N |
| SMILES | CC(CCN1C=CC(=CC1=O)C2=C(C=C(C=C2)OC)F)(C(=O)NO)S(=O)(=O)C |
| Reference | [1]. Tomaras AP, et al. LpxC inhibitors as new antibacterial agents and tools for studying regulation of lipid A biosynthesis in Gram-negative pathogens. mBio. 2014 Sep 30;5(5):e01551-14. [2]. García-Quintanilla M, et al. Inhibition of LpxC Increases Antibiotic Susceptibility in Acinetobacter baumannii. Antimicrob Agents Chemother. 2016 Jul 22;60(8):5076-9. |
