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| Targets |
Fleroxacin targets bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, enzymes that are essential for bacterial DNA replication, transcription, and repair. By inhibiting these enzymes, fleroxacin prevents DNA supercoiling and separation, leading to DNA damage and bacterial cell death. The compound's trifluoroquinolone structure contributes to its potent antibacterial activity.
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| ln Vitro |
Fleroxacin is a broad-spectrum antibiotic with activity against a wide range of Gram-positive and Gram-negative bacteria. It has been shown to be effective against Neisseria gonorrhoeae, enteric pathogens, respiratory pathogens, and urinary tract pathogens. The compound's antibacterial activity is assessed using standard broth microdilution or agar dilution methods to determine MIC values.
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| ln Vivo |
A new trifluoroquinolone with strong action against a wide range of Gram-positive and Gram-negative bacteria is called fleroxacin (Ro 23-6240). The lengthy elimination half-life (9 to 10 hours) and high plasma concentrations (e.g., maximum concentration of 2.3 μg/ml following an oral dose of 200 mg) are characteristics of the pharmacokinetics of fleroxacin [1]. In vitro, froxacin (Ro 23-6240) effectively combats Haemophilus ducreyi. In patients who are not co-infected with HIV-1, froxacin (Ro 23-6240), 200 or 400 mg as a single oral dose, is efficacious in treating microbiologically confirmed chancre. A single 200 or 400 mg dose of fleroxacin is not enough to treat chancroid in men with HIV-1 infection [2][3].
Fleroxacin is used in vivo for the treatment of various bacterial infections. It is available in both oral and intravenous formulations and is reportedly useful in the treatment of gonorrhea, bacterial enteritis, chronic bronchitis, and urinary tract infections. It is also used for skin and soft tissue infections and intra-abdominal infections. |
| Enzyme Assay |
For non-cellular enzyme assays, fleroxacin's inhibition of DNA gyrase and topoisomerase IV can be evaluated using purified enzymes in cell-free systems. The DNA supercoiling activity of DNA gyrase is measured by monitoring the conversion of relaxed plasmid DNA to supercoiled DNA using agarose gel electrophoresis. IC₅₀ values are determined by incubating varying concentrations of fleroxacin with the enzyme and DNA substrate.
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| Cell Assay |
In vitro cellular assays for fleroxacin involve treating bacterial cultures with the compound and assessing growth inhibition. The minimum inhibitory concentration (MIC) is determined by broth microdilution according to CLSI guidelines. Time-kill assays are used to assess the bactericidal activity of the compound. The compound's effect on bacterial DNA synthesis can be assessed by measuring the incorporation of [³H]-thymidine.
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| Animal Protocol |
In vivo animal experiments with fleroxacin involve administering the compound to animal models of bacterial infection. Mice or rats are infected with a pathogenic bacterium (e.g., S. aureus or E. coli) and treated with fleroxacin orally or intravenously. The compound's efficacy is assessed by measuring survival rates, bacterial load in tissues, and resolution of clinical signs of infection.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
After oral administration, it can be rapidly and well absorbed from the gastrointestinal tract. Fleroxacin has a molecular weight of 369.34 and a molecular formula of C₁₇H₁₈F₃N₃O₃. It is a white crystalline powder with a purity of ≥98%. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions and is typically stored at room temperature. Pharmacokinetic studies show that it has good oral bioavailability and a long half-life, supporting once-daily dosing. |
| Toxicity/Toxicokinetics |
Fleroxacin is generally well-tolerated, but like other fluoroquinolones, it can cause gastrointestinal disturbances, central nervous system effects (headache, dizziness), and phototoxicity. It may also cause tendonitis and tendon rupture, particularly in older patients. The compound should be used with caution in patients with renal impairment and should be avoided in children and pregnant women due to effects on cartilage development.
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| References |
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| Additional Infomation |
Fleroxacin is a fluoroquinolone antibiotic with the chemical name 4-oxo-1,4-dihydroquinoline, in which the 1, 3, 6, 7, and 8 positions are substituted with 2-fluoroethyl, carboxyl, fluorine, 4-methylpiperazin-1-yl, and fluorine atoms, respectively. It is active against a variety of Gram-positive and Gram-negative bacteria. Fleroxacin is a topoisomerase IV inhibitor, an antibacterial drug, and an EC 5.99.1.3 [DNA topoisomerase (ATP hydrolysis)] inhibitor. It belongs to the quinoline class, fluoroquinolone class of antibiotics, difluorobenzene class, N-alkylpiperazine class, and monocarboxylic acid class of compounds. Fleroxacin is a broad-spectrum antibacterial fluoroquinolone drug. It potently inhibits the DNA supercoiling activity of DNA gyrase. Fleroxacin is not a CYP1A2 inhibitor. A broad-spectrum antibacterial fluoroquinolone drug. This drug potently inhibits the DNA supercoiling activity of DNA gyrase. Drug Indications Fleroxacin is a broad-spectrum antibacterial fluoroquinolone. Mechanism of Action Inhibition of DNA gyrase and DNA topoisomerase 2 ultimately leads to cell death, as these enzymes are essential for bacterial DNA replication, transcription, repair, supercoiling repair, and recombination. Pharmacodynamics Fleroxacin is a broad-spectrum antibacterial fluoroquinolone. It potently inhibits the DNA supercoiling activity of DNA gyrase.
Fleroxacin is a trifluoroquinolone antibiotic used for the treatment of various bacterial infections. It is available in both oral and intravenous formulations and is reportedly useful in the treatment of gonorrhea, bacterial enteritis, chronic bronchitis, and urinary tract infections. The compound's mechanism of action involves inhibition of bacterial DNA gyrase and topoisomerase IV. |
| Molecular Formula |
C17H18F3N3O3
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| Molecular Weight |
369.3383
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| Exact Mass |
369.13
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| CAS # |
79660-72-3
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| PubChem CID |
3357
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
535.3±50.0 °C at 760 mmHg
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| Melting Point |
264-266°C
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| Flash Point |
277.6±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.568
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| LogP |
1.72
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
595
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XBJBPGROQZJDOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18F3N3O3/c1-21-4-6-22(7-5-21)15-12(19)8-10-14(13(15)20)23(3-2-18)9-11(16(10)24)17(25)26/h8-9H,2-7H2,1H3,(H,25,26)
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| Chemical Name |
6,8-difluoro-1-(2-fluoroethyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
0.1 M NaOH : ~9.17 mg/mL (~24.83 mM)
H2O : ~1 mg/mL (~2.71 mM) DMSO :< 1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7075 mL | 13.5377 mL | 27.0753 mL | |
| 5 mM | 0.5415 mL | 2.7075 mL | 5.4151 mL | |
| 10 mM | 0.2708 mL | 1.3538 mL | 2.7075 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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