Fabimycin
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo.
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- No. CAS: 2651965-71-6
- Fòrmula: C23H25ClN4O3
- Peso molecular:440.92
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Fabimycin shows outstanding activity against S. aureus (MIC: 4 ng/mL), E. coli MG1655 (MIC: 2 μg/mL)[1].
Fabimycin (4 μg/mL) inhibits 90% of the strainsagainst a panel of 100 K. pneumoniae clinical isolates[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fabimycin (intraperitoneal injection) is tolerated in mice with an MTD of >200 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute pneumonia murine or neutropenic mouse thigh infection model, initiated in CD-1 mice with A. baumannii[1]
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Dosage:50 mg/kg
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Administration:Intramuscular injection, 4, 23, and 41 h postinfection (pneumonia model), or 2, 6, and 11 h postinfection (thigh infection)
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Result:Achieved a >3‑fold decrease in log(CFU/lung) and >2-fold decrease log(CFU/thigh) relative to the vehicle.
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Animal Model:Urinary tract infections (UTIs) model (C3H/HeJ mice)[1]
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Dosage:33.3 mg/kg
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Administration:Intravenous injection, three times a day,
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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.
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Animal Model:Neutropenic female BALB/c mice infected with drug-resistant A. baumannii (pharmacokinetic assay)[1]
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Dosage:20, 50, 75, 100 mg/kg
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Administration:Intravenous injection, for a single dose
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Result:Pharmacokinetic profile of Fabimycin.
pharmacokinetic property AUClast (h•μg/mL) T1/2 (h) CL (mL/min/kg) Cmax (μg/mL) 100 mg/kg 69.8 1.4 23.5 47.3 75 mg/kg 45.4 1.4 26.9 34.6
Chemical Information
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No. CAS 2651965-71-6
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Peso molecular 440.92
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Fòrmula C23H25ClN4O3
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SMILES
O=C(/C=C/C(C=C1CC[C@@H]2[NH3+])=CN=C1NC2=O)N(C)CC(O3)=C(C)C4=C3C=CC=C4.[Cl-]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)