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编 号：F754410
分子式：C23H25ClN4O3
分子量：440.92
分子式：C23H25ClN4O3
分子量：440.92
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CAS No: 2651965-71-6
产品详情
生物活性：
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo.
体内研究：
Fabimycin (Intramuscular injection, 5 mg/kg, 2 and 7 h postinfection) shows significant great reduction of bacterial burden in Neutropenic mouse thigh infection initiated in CD-1 mice with S. aureus.Fabimycin (intraperitoneal injection) is tolerated in mice with an MTD of >200 mg/kg.Animal Model:Acute pneumonia murine or neutropenic mouse thigh infection model, initiated in CD-1 mice with A. baumannii
Dosage:50 mg/kg
Administration:Intramuscular injection, 4, 23, and 41 h postinfection (pneumonia model), or 2, 6, and 11 h postinfection (thigh infection)
Result:Achieved a >3?fold decrease in log(CFU/lung) and >2-fold decrease log(CFU/thigh) relative to the vehicle.
Animal Model:Urinary tract infections (UTIs) model (C3H/HeJ mice)
Dosage:33.3 mg/kg
Administration:Intravenous injection, three times a day,
Result:Achieved 3.0, 2.8, 2.9, and 1.9 log10 reductions in bacterial load relative to the vehicle in the spleen, bladder, liver, and kidney tissues, respectively.
Animal Model:Neutropenic female BALB/c mice infected with drug-resistant A. baumannii (pharmacokinetic assay)
Dosage:20, 50, 75, 100 mg/kg
Administration:Intravenous injection, for a single dose
Result:Pharmacokinetic profile of Fabimycin.pharmacokinetic property AUClast (h?μg/mL) T1/2 (h)CL (mL/min/kg) Cmax (μg/mL)
100 mg/kg 69.81.423.547.3
75 mg/kg 45.41.426.934.6
体外研究：
Fabimycin shows outstanding activity against S. aureus (MIC: 4 ng/mL),E. coli MG1655 (MIC: 2 μg/mL).Fabimycin (4 μg/mL) inhibits 90% of the strainsagainst a panel of 100 K. pneumoniae clinical isolates.Fabimycin enhances the stability of the enzyme-inhibitor complex significantly more than the less active enantiomer in both E. coli and A. baumannii versions of FabI.
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo.
体内研究：
Fabimycin (Intramuscular injection, 5 mg/kg, 2 and 7 h postinfection) shows significant great reduction of bacterial burden in Neutropenic mouse thigh infection initiated in CD-1 mice with S. aureus.Fabimycin (intraperitoneal injection) is tolerated in mice with an MTD of >200 mg/kg.Animal Model:Acute pneumonia murine or neutropenic mouse thigh infection model, initiated in CD-1 mice with A. baumannii
Dosage:50 mg/kg
Administration:Intramuscular injection, 4, 23, and 41 h postinfection (pneumonia model), or 2, 6, and 11 h postinfection (thigh infection)
Result:Achieved a >3?fold decrease in log(CFU/lung) and >2-fold decrease log(CFU/thigh) relative to the vehicle.
Animal Model:Urinary tract infections (UTIs) model (C3H/HeJ mice)
Dosage:33.3 mg/kg
Administration:Intravenous injection, three times a day,
Result:Achieved 3.0, 2.8, 2.9, and 1.9 log10 reductions in bacterial load relative to the vehicle in the spleen, bladder, liver, and kidney tissues, respectively.
Animal Model:Neutropenic female BALB/c mice infected with drug-resistant A. baumannii (pharmacokinetic assay)
Dosage:20, 50, 75, 100 mg/kg
Administration:Intravenous injection, for a single dose
Result:Pharmacokinetic profile of Fabimycin.pharmacokinetic property AUClast (h?μg/mL) T1/2 (h)CL (mL/min/kg) Cmax (μg/mL)
100 mg/kg 69.81.423.547.3
75 mg/kg 45.41.426.934.6
体外研究：
Fabimycin shows outstanding activity against S. aureus (MIC: 4 ng/mL),E. coli MG1655 (MIC: 2 μg/mL).Fabimycin (4 μg/mL) inhibits 90% of the strainsagainst a panel of 100 K. pneumoniae clinical isolates.Fabimycin enhances the stability of the enzyme-inhibitor complex significantly more than the less active enantiomer in both E. coli and A. baumannii versions of FabI.
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