1. Anti-infection
  2. Antibiotic Bacterial
  3. PF-5081090

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.

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PF-5081090 Chemical Structure

PF-5081090 Chemical Structure

CAS No. : 1312473-63-4

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Description

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].

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)[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

412.43

Formula

C18H21FN2O6S

CAS No.
SMILES

FC1=C(C2=CC(N(CC[C@](S(C)(=O)=O)(C)C(NO)=O)C=C2)=O)C=CC(OC)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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PF-5081090 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PF-5081090
Cat. No.:
HY-103251
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