Difloxacin
Difloxacin (A-56619) is an orally active bactericidal agent. Difloxacin inhibits bacterial DNA gyrase. Difloxacin exhibits concentration-dependent bactericidal activity. Difloxacin shows strong in vitro activity against a variety of Gram-positive and Gram-negative bacteria. Difloxacin can be used in research related to colibacillosis and Staphylococcus aureus infections.
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- CAS. Nr.: 98106-17-3
- Formel: C21H19F2N3O3
- Molecular Weight:399.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Difloxacin (24-48 h) inhibits and eliminates the field strain of E. coli O78 in vitro with an MIC of 0.02 µg/mL and an MBC of 0.04 µg/mL[1].
Difloxacin (0.04-12.5 µg/mL) exhibits 3.99% protein binding in normal chicken serum in vitro[1].
Difloxacin exhibits broad-spectrum in vitro antibacterial activity against clinical isolates of gram-positive (Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus faecalis) and gram-negative (Escherichia coli, Klebsiella pneumoniae, Salmonella typhimurium, Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Providencia stuartii, Pseudomonas aeruginosa) bacteria[2].
Difloxacin (1-25 μg/mL; 72 h) dose-dependently and reversibly inhibits ConA-induced proliferation of human peripheral blood mononuclear cells, with maximum inhibition when added within the first 24 h of culture, 92% cell viability at 25 μg/mL, and no reversal of inhibition with increased mitogen concentration[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Difloxacin (administered via subcutaneous injection or oral route; twice daily; at 1 h and 5 h post-infection) exhibits an ED50 of 1.7 mg/kg per day for subcutaneous administration and 3.2 mg/kg per day for oral administration against lethal Staphylococcus aureus 10649 infection in CF-1 mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:1.7 mg/kg per day (subcutaneous); 3.2 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 1.7 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 3.2 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:5.2 mg/kg per day (subcutaneous); 8.7 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 5.2 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 8.7 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:14.9 mg/kg per day (subcutaneous); 19.6 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 14.9 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 19.6 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:2.2 mg/kg per day (subcutaneous); 3.9 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 2.2 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 3.9 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:0.5 mg/kg per day (subcutaneous); 1.1 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 0.5 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 1.1 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:1.6 mg/kg per day (subcutaneous); 1.4 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 24 and 28 h; oral; twice daily; post-infection at 24 and 28 h
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Result:Achieved an ED50 of 1.6 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 1.4 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:2.9 mg/kg per day (subcutaneous); 7.3 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 2.9 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 7.3 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:4.2 mg/kg per day (subcutaneous); 14.9 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 4.2 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 14.9 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:1.5 mg/kg per day (subcutaneous); 1.9 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 1.5 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 1.9 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:3.7 mg/kg per day (subcutaneous); 4.9 mg/kg per day (oral)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 3.7 mg/kg per day via subcutaneous administration.
Achieved an ED50 of 4.9 mg/kg per day via oral administration.
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Animal Model:CF-1 (female, 20 g)[2]
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Dosage:5.2 mg/kg per day (subcutaneous)
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Administration:subcutaneous; twice daily; post-infection at 1 and 5 h
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Result:Achieved an ED50 of 5.2 mg/kg per day via subcutaneous administration.
Chemical Information
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CAS. Nr. 98106-17-3
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Molecular Weight 399.39
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Formel C21H19F2N3O3
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SMILES
O=C(C1=CN(C2=CC=C(F)C=C2)C3=C(C=C(F)C(N4CCN(C)CC4)=C3)C1=O)O
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Synonyms
A-56619
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Abo El-Ela FI, et al. Pharmacokinetics of difloxacin in healthy and E. coli-infected broiler chickens. Br Poult Sci. 2014;55(6):830-836. [Content Brief]
[2]. Fernandes PB, et al. In vivo evaluation of A-56619 (difloxacin) and A-56620: new aryl-fluoroquinolones. Antimicrob Agents Chemother. 1986;29(2):201-208. [Content Brief]
[3]. Gollapudi SV, et al. Aryl-fluoroquinolone derivatives A-56619 (difloxacin) and A-56620 inhibit mitogen-induced human mononuclear cell proliferation. Antimicrob Agents Chemother. 1986;30(3):390-394. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Difloxacin Related Classifications
HY-121272 Related Classifications
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Keywords
- Difloxacin
- 98106-17-3
- A-56619
- A56619
- A 56619
- Bacterial
- DNA/RNA Synthesis
- bacterial DNA gyrase
- Escherichia coli
- Gram-positive bacteria
- mammalian topoisomerase II
- Gram-negative bacteria
- bacterial topoisomerase IV
- eucaryotic alpha DNA polymerases
- eucaryotic beta DNA polymerases
- mycoplasma
- human peripheral blood mononuclear cells
- Inhibitor
- inhibitor
- inhibit