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 No.: 98106-17-3
- Formule: C21H19F2N3O3
- Masse moléculaire:399.39
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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. Further protocols information, click here.
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 No. 98106-17-3
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Masse moléculaire 399.39
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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