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  3. Difloxacin hydrochloride

Difloxacin hydrochloride  (Synonyms: A-56619 hydrochloride)

Cat. No.: HY-N7066 Purity: 99.52%
Handling Instructions Technical Support

Difloxacin hydrochloride (A-56619 hydrochloride) is an orally active bactericidal agent. Difloxacin hydrochloride inhibits bacterial DNA gyrase. Difloxacin hydrochloride exhibits concentration-dependent bactericidal activity. Difloxacin hydrochloride shows strong in vitro activity against a variety of Gram-positive and Gram-negative bacteria. Difloxacin hydrochloride can be used in research related to colibacillosis and *Staphylococcus aureus* infections.

For research use only. We do not sell to patients.

Difloxacin hydrochloride

Difloxacin hydrochloride Chemical Structure

CAS No. : 91296-86-5

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Description

Difloxacin hydrochloride (A-56619 hydrochloride) is an orally active bactericidal agent. Difloxacin hydrochloride inhibits bacterial DNA gyrase. Difloxacin hydrochloride exhibits concentration-dependent bactericidal activity. Difloxacin hydrochloride shows strong in vitro activity against a variety of Gram-positive and Gram-negative bacteria. Difloxacin hydrochloride can be used in research related to colibacillosis and *Staphylococcus aureus* infections[1][2][3].

In Vitro

Difloxacin (24-48 h) hydrochloride 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) hydrochloride exhibits 3.99% protein binding in normal chicken serum in vitro[1].
Difloxacin hydrochloride 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) hydrochloride 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.

Parmacokinetics
Species Dose Route Vss CLtotal AUC MRT T1/2 (Elimination) Tmax Cmax Bioavailability
Chicken[1] 10 mg/kg i.v. 3.14 L/kg 0.65 mL/h/kg 15.19 μg·h/mL 4.73 h / / / /
Chicken[1] 10 mg/kg p.o. / / 12.16 μg·h/mL 7.66 h 4.70 h 2.27 h 1.34 μg/mL 86.24 %
In Vivo

The serum concentration of difloxacin (10 mg/kg; intravenous injection, oral administration; single dose) hydrochloride in healthy broilers remains sustainably above the MIC of E. coli, with an oral bioavailability as high as 86.2% and an elimination half-life of 3.7 h following intravenous injection[1].
Difloxacin (administered via subcutaneous injection or oral route; twice daily; at 1 h and 5 h post-infection) hydrochloride 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.

Animal Model: CF-1 (female, 20 g)[2]
Dosage: 1.7 mg/kg per day (subcutaneous); 3.2 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 5.2 mg/kg per day (subcutaneous); 8.7 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 14.9 mg/kg per day (subcutaneous); 19.6 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 2.2 mg/kg per day (subcutaneous); 3.9 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 0.5 mg/kg per day (subcutaneous); 1.1 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 1.6 mg/kg per day (subcutaneous); 1.4 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 24 and 28 h; oral; twice daily; post-infection at 24 and 28 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 2.9 mg/kg per day (subcutaneous); 7.3 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 4.2 mg/kg per day (subcutaneous); 14.9 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 1.5 mg/kg per day (subcutaneous); 1.9 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 3.7 mg/kg per day (subcutaneous); 4.9 mg/kg per day (oral)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h; oral; twice daily; post-infection at 1 and 5 h
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.
Animal Model: CF-1 (female, 20 g)[2]
Dosage: 5.2 mg/kg per day (subcutaneous)
Administration: subcutaneous; twice daily; post-infection at 1 and 5 h
Result: Achieved an ED50 of 5.2 mg/kg per day via subcutaneous administration.
Molecular Weight

435.85

Formula

C21H20ClF2N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2=CC=C(F)C=C2)C3=C(C=C(F)C(N4CCN(C)CC4)=C3)C1=O)O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 5 mg/mL (11.47 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.52%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.2944 mL 11.4718 mL 22.9437 mL 57.3592 mL
5 mM 0.4589 mL 2.2944 mL 4.5887 mL 11.4718 mL
10 mM 0.2294 mL 1.1472 mL 2.2944 mL 5.7359 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Difloxacin hydrochloride
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