| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| 10g | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Bacterial DNA gyrase (inhibition of DNA gyrase is the principal mechanism of action). [1]
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| ln Vitro |
Danofloxacin is a synthetic antibacterial agent of the fluoroquinolone class, acts principally by the inhibition of bacterial DNA-gyrase, which is necessary for supercoiling of DNA to provide a suitable spatial arrangement of DNA within the bacterial cell. The minimum inhibitory concentration of danofloxacin against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica, Pasteurella multocida and Haemophilus somnus, the most important bacterial respiratory pathogens of cattle, is 0.125 μg/ml.
The minimum inhibitory concentration (MIC) of Danofloxacin Mesylate against 90% (MIC90) of contemporary European and North American field isolates of Pasteurella haemolytica was 0.125 μg/mL (Europe) and 0.06 μg/mL (North America); MIC90 against Pasteurella multocida was 0.06 μg/mL for both origins; MIC90 against Haemophilus somnus was 0.06 μg/mL for both origins. MIC range for all isolates was ≤0.008 μg/mL to 2 μg/mL. [1] In comparison, MIC90 values of other antibacterials (oxytetracycline, trimethoprim/sulphamethoxazole, amoxycillin, erythromycin) against these isolates were generally much higher (e.g., oxytetracycline MIC90 >64 μg/mL for many Pasteurella isolates). [1] |
| ln Vivo |
Danofloxacin shows protective dose (PD50) of 0.38, 0.8, 2.42 mg/kg for P. multocida, E. coli and S. choleraesuis in in vivo mouse protection assay.
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| Animal Protocol |
Dissolved in 2.5% or 5% water solution; 0-10 mg/kg; p.o or s.c. Mice model
Kinetics study I: Twelve cross-bred calves (90-133 kg) were used in a cross-over design. On day 0, a single intravenous (IV) injection of Danofloxacin Mesylate at 1.25 mg/kg was given to group A; subcutaneous (SC) injection at 1.25 mg/kg to group B; intramuscular (IM) injection at 1.25 mg/kg to group C. Blood samples were collected at 0.25, 0.5, 1, 2, 4, 6, 8, 12, and 24 h post-dose. Groups B and C then received four more daily doses (SC or IM) at 24-h intervals, with blood sampling repeated on days 2 and 4. The treatment and sampling were repeated on days 12 and 24 with routes rotated. Calves were re-weighed on days 12 and 24 to recalculate dose. [1] Kinetics study II: Thirty-six cross-bred calves (223-291 kg) received a single IM injection of Danofloxacin Mesylate at 1.25 mg/kg. Groups of calves were slaughtered at 1, 2, 4, 8, 12, and 24 h post-dose. Before slaughter, heparinized blood samples were collected from the jugular vein. After slaughter, lungs were removed, and pooled lung tissue samples (approx. 500 g per calf) were homogenized and aliquots stored for analysis. [1] |
| ADME/Pharmacokinetics |
After IV administration at 1.25 mg/kg, plasma concentrations declined biexponentially with a terminal elimination half-life (t1/2) of 4.01 h (harmonic mean), systemic plasma clearance (CLp) of 0.468 L/h·kg, volume of distribution at steady state (Vdss) of 2.48 L/kg. [1]
After IM administration at 1.25 mg/kg, mean Cmax in plasma was 0.47 μg/mL (first dose), Tmax ~1.0 h, AUC(0-∞) 2.8 μg·h/mL, t1/2 ~3.86 h. After SC administration, mean Cmax was 0.37 μg/mL, AUC(0-∞) 2.6 μg·h/mL. Bioavailability was 101% (IM) and 94% (SC) relative to IV. No significant differences in AUC between routes; IM gave higher Cmax (statistically significant for first and third doses). [1] After a single IM dose of 1.25 mg/kg, mean peak lung concentration was 1.44 μg/g, which was 4.1 times greater than peak plasma concentration (0.35 μg/mL). Tmax for both lung and plasma was 1.0 h. AUC(0-∞) for lung was 7.4 μg·h/g, 3.7 times greater than that for plasma (2.0 μg·h/mL). Elimination half-life from lung (peak to 12 h) was 3.5 h, similar to plasma (3.3 h). A slower later elimination phase in lung with t1/2 ~4.3 h was suggested. [1] Plasma protein binding of Danofloxacin Mesylate was concentration-dependent: 50±3% at 50 ng/mL, 42±3% at 100 ng/mL, 34±1% at 250 ng/mL, 29±1% at 500 ng/mL, and 26±1% at 1000 ng/mL. [1] |
| Toxicity/Toxicokinetics |
Safety evaluation in various age groups of cattle in laboratory and field studies demonstrated that Danofloxacin Mesylate injectable has a wide margin of safety when the recommended dose is administered by IM or SC routes. No adverse effects were observed in field usage, and no adverse effects upon reproductive performance were observed following treatment of breeding cattle. [1]
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| References |
J Vet Pharmacol Ther.1991 Dec;14(4):400-10;J Med Chem.1992 Feb 21;35(4):611-20.
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| Additional Infomation |
Danofloxacin mesylate belongs to the quinoline class of compounds.
Danofloxacin Mesylate is a fluoroquinolone antibacterial developed for veterinary use. Its mechanism of action is inhibition of bacterial DNA gyrase. It is indicated for the treatment of bacterial respiratory disease in cattle, particularly against Pasteurella haemolytica, Pasteurella multocida, and Haemophilus somnus. The MIC90 values against these pathogens (0.06-0.125 μg/mL) are substantially lower than the plasma and lung concentrations achieved after parenteral administration of 1.25 mg/kg, supporting clinical efficacy. [1] |
| Molecular Formula |
C19H20FN3O3.CH4O3S
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|---|---|
| Molecular Weight |
453.48
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| Exact Mass |
453.136
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| Elemental Analysis |
C, 52.97; H, 5.33; F, 4.19; N, 9.27; O, 21.17; S, 7.07
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| CAS # |
119478-55-6
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| Related CAS # |
Danofloxacin;112398-08-0;Danofloxacin-d3 mesylate;1217860-94-0
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| PubChem CID |
71334
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| Appearance |
Solid powder
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| Boiling Point |
569.3ºC at 760 mmHg
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| Melting Point |
337-339ºC
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| Flash Point |
298.1ºC
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| Vapour Pressure |
8.41E-14mmHg at 25°C
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| LogP |
2.654
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
772
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| Defined Atom Stereocenter Count |
2
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| SMILES |
S(C([H])([H])[H])(=O)(=O)O[H].FC1C([H])=C2C(C(C(=O)O[H])=C([H])N(C2=C([H])C=1N1C([H])([H])[C@]2([H])C([H])([H])[C@@]1([H])C([H])([H])N2C([H])([H])[H])C1([H])C([H])([H])C1([H])[H])=O
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| InChi Key |
APFDJSVKQNSTKF-FXMYHANSSA-N
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| InChi Code |
InChI=1S/C19H20FN3O3.CH4O3S/c1-21-7-12-4-11(21)8-22(12)17-6-16-13(5-15(17)20)18(24)14(19(25)26)9-23(16)10-2-3-10;1-5(2,3)4/h5-6,9-12H,2-4,7-8H2,1H3,(H,25,26);1H3,(H,2,3,4)/t11-,12-;/m0./s1
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| Chemical Name |
1-Cyclopropyl-6-fluoro-1,4-dihydro-7-((1S,4S)-5-methyl-2,5-diazabicyclo(2.2.1)hept-2-yl)-4-oxo-3-quinolinecarboxylic acid, monomethanesulfonate
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| Synonyms |
CP 76,136-27; CP-76,136-27; Danofloxacin monomethanesulfonate.
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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) |
Water : 91~100 mg/mL(~220.52 mM)
DMSO : ~20 mg/mL (~44.10 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (4.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: Saline: 30 mg/mL Solubility in Formulation 5: 50 mg/mL (110.26 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2052 mL | 11.0258 mL | 22.0517 mL | |
| 5 mM | 0.4410 mL | 2.2052 mL | 4.4103 mL | |
| 10 mM | 0.2205 mL | 1.1026 mL | 2.2052 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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