| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Difloxacin HCl targets bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, which are essential enzymes for bacterial DNA replication, transcription, and repair. By inhibiting these enzymes, difloxacin prevents the supercoiling and relaxation of bacterial DNA, leading to the inhibition of DNA replication and ultimately bacterial cell death. The compound specifically targets the A subunit of DNA gyrase. It displays concentration-dependent bactericidal activity.
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| ln Vitro |
In vitro, difloxacin HCl exhibits broad-spectrum antibacterial activity against a variety of bacterial pathogens. It is effective against Gram-positive bacteria such as Staphylococcus species and Gram-negative bacteria such as Escherichia coli and Pasteurella species. Minimum inhibitory concentrations (MICs) vary depending on the organism. The compound's antibacterial activity has been demonstrated in standard microbiological susceptibility tests, confirming its efficacy against susceptible bacteria.
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| ln Vivo |
In vivo, difloxacin HCl is used in veterinary medicine for the treatment of bacterial infections. It is marketed under the brand name Dicural for veterinary applications. The compound's efficacy has been demonstrated in clinical studies in food animals. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. Difloxacin HCl is administered orally and is effective against a range of susceptible bacterial pathogens.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for difloxacin HCl are not typically performed because the compound's antibacterial activity is assessed using microbiological methods. However, the compound's mechanism of action can be studied using assays that measure its ability to inhibit DNA gyrase or topoisomerase IV. In these assays, purified bacterial DNA gyrase or topoisomerase IV is incubated with DNA substrate and ATP in the presence of varying concentrations of difloxacin, and the extent of DNA supercoiling or relaxation is measured.
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| Cell Assay |
In vitro cellular assays for difloxacin HCl are performed using standard microbiological susceptibility testing methods. The minimum inhibitory concentration (MIC) is determined using broth dilution or agar dilution methods according to Clinical and Laboratory Standards Institute (CLSI) guidelines. Susceptibility testing is performed using a range of bacterial strains, including both Gram-positive and Gram-negative organisms. The zone of inhibition can also be measured using disk diffusion assays. These assays confirm the antibacterial activity of difloxacin HCl.
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| Animal Protocol |
In vivo animal experiments for difloxacin HCl are conducted in target animal species such as poultry, swine, and cattle to evaluate its efficacy in treating bacterial infections. Animals are infected with a bacterial pathogen (e.g., Escherichia coli, Pasteurella) and then treated with difloxacin HCl via oral administration or incorporation into feed or water. The primary endpoints include survival, bacterial clearance from tissues, and improvement in clinical signs. These studies support the compound's approval for veterinary use.
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| ADME/Pharmacokinetics |
Difloxacin HCl has a molecular weight of 435.85 and a molecular formula of C21H19N3O3F2·HCl. The compound is a white to off-white solid powder with a melting point >245°C (dec.). It is soluble in water (~5 mg/mL) and DMSO. The compound should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. For in vivo administration, it can be formulated in various vehicles.
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| Toxicity/Toxicokinetics |
Difloxacin HCl has been evaluated in veterinary toxicology studies. As a fluoroquinolone antibiotic, it may cause adverse effects including gastrointestinal disturbances and, rarely, cartilage damage in juvenile animals. The compound is approved for use in food animals with appropriate withdrawal periods to ensure food safety. No significant toxicity has been reported at therapeutic doses in target animal species.
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| Additional Infomation |
Difloxacin hydrochloride belongs to the quinoline class of drugs.
Difloxacin HCl is a fluoroquinolone antibiotic developed for veterinary use, marketed under the brand name Dicural. It is used to treat bacterial infections in food animals, including poultry, swine, and cattle. The compound inhibits bacterial DNA gyrase and topoisomerase IV, displaying concentration-dependent bactericidal activity. Difloxacin HCl is not approved for human use in many countries. It is a research compound for veterinary applications. |
| Molecular Formula |
C21H19N3O3F2.HCL
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|---|---|
| Molecular Weight |
435.8516
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| Exact Mass |
435.116
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| CAS # |
91296-86-5
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| Related CAS # |
Difloxacin-d3 hydrochloride;1173021-89-0;Difloxacin;98106-17-3
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| PubChem CID |
56205
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| Appearance |
White to off-white solid powder
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| Density |
1.409 g/cm3
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| Boiling Point |
595.5ºC at 760 mmHg
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| Melting Point |
>245ºC (dec.)
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| Flash Point |
313.9ºC
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| Index of Refraction |
1.629
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| LogP |
3.523
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
672
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C(C1C(=O)C2C(=CC(N3CCN(C)CC3)=C(C=2)F)N(C2C=CC(F)=CC=2)C=1)O
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| InChi Key |
JFMGBGLSDVIOHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F2N3O3.ClH/c1-24-6-8-25(9-7-24)19-11-18-15(10-17(19)23)20(27)16(21(28)29)12-26(18)14-4-2-13(22)3-5-14;/h2-5,10-12H,6-9H2,1H3,(H,28,29);1H
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| Chemical Name |
6-fluoro-1-(4-fluorophenyl)-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;hydrochloride
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~5 mg/mL (~11.47 mM)
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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 | 2.2944 mL | 11.4718 mL | 22.9437 mL | |
| 5 mM | 0.4589 mL | 2.2944 mL | 4.5887 mL | |
| 10 mM | 0.2294 mL | 1.1472 mL | 2.2944 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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