| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g | |||
| 5g | |||
| Other Sizes |
| Targets |
Quinolone
Danofloxacin functions as an antimicrobial agent by inhibiting bacterial DNA gyrase (also known as topoisomerase II), an essential enzyme for bacterial DNA replication. By binding to the DNA gyrase enzyme, it prevents the supercoiling of bacterial DNA, which is necessary for transcription and replication. This inhibition ultimately leads to the cessation of bacterial cell division and cell death. As a third-generation fluoroquinolone, Danofloxacin exhibits a wide range of activity against the majority of Gram-positive and Gram-negative bacteria, as well as against mycoplasma and chlamydia species. Its primary target is the bacterial DNA gyrase, which is a validated target for antibacterial therapy in veterinary medicine. |
|---|---|
| ln Vitro |
Danofloxacin demonstrates broad-spectrum antibacterial activity in vitro against a wide range of pathogens. It is effective against most Gram-positive and Gram-negative bacteria, mycoplasma, and chlamydia species. As a fluoroquinolone antibiotic, it functions by inhibiting bacterial DNA gyrase, thereby blocking DNA replication. The compound shows potent activity against veterinary pathogens, including those responsible for respiratory diseases in livestock. Its in vitro activity is characterized by low minimum inhibitory concentrations (MICs) against susceptible bacterial strains. Danofloxacin is slightly soluble in water, which may affect its formulation for in vitro susceptibility testing.
|
| ln Vivo |
Danofloxacin exhibits potent in vivo antibacterial activity in animal models of infection. It has been used for the prevention and treatment of respiratory diseases in cattle, pigs, and chickens. As an orally active antibiotic, it is effective against systemic and respiratory infections caused by susceptible Gram-positive and Gram-negative bacteria. The compound was developed by Pfizer and introduced in 1991 for the treatment of various veterinary pathogens. Its in vivo efficacy is attributed to its ability to achieve therapeutic concentrations in target tissues, including the lungs, and its broad-spectrum activity against common veterinary pathogens.
|
| Enzyme Assay |
Danofloxacin's antibacterial activity is primarily mediated through the inhibition of bacterial DNA gyrase, an enzyme critical for DNA replication. In vitro enzyme assays typically involve measuring the inhibition of DNA gyrase supercoiling activity or the relaxation of supercoiled DNA. The compound is tested against purified bacterial DNA gyrase enzymes from susceptible strains, and the inhibition is quantified by determining the concentration required to inhibit 50% of the enzyme activity (IC50). These assays confirm the mechanism of action as a topoisomerase inhibitor. The binding of Danofloxacin to the DNA gyrase-DNA complex stabilizes the enzyme-DNA cleavage complex, leading to the accumulation of double-strand breaks and ultimately bacterial cell death.
|
| Cell Assay |
In vitro cellular assays for Danofloxacin typically involve assessing its antibacterial activity against a panel of veterinary pathogens, including Gram-positive and Gram-negative bacteria, mycoplasma, and chlamydia species. The standard assay format is the broth microdilution method to determine the minimum inhibitory concentration (MIC). Bacterial cultures are grown in appropriate media and exposed to serial dilutions of the compound. After incubation, the MIC is determined as the lowest concentration that inhibits visible bacterial growth. Time-kill kinetics assays may also be performed to evaluate the bactericidal activity of the compound. These cell-based assays are essential for characterizing the antimicrobial spectrum and potency of Danofloxacin against clinically relevant veterinary isolates.
|
| Animal Protocol |
In vivo animal models for Danofloxacin typically involve inducing bacterial infections in target species such as cattle, pigs, or chickens, followed by oral administration of the compound. Efficacy is assessed by monitoring clinical signs, survival rates, and bacterial load reduction in infected tissues. Pharmacokinetic/pharmacodynamic (PK/PD) studies are often conducted to correlate drug exposure with therapeutic outcome. The compound is administered orally, and plasma and tissue concentrations are measured to establish dose-response relationships. These studies help determine the optimal dosing regimens for treating respiratory and systemic infections in veterinary practice.
|
| ADME/Pharmacokinetics |
Danofloxacin exhibits favorable pharmacokinetic properties in veterinary species. It is slightly soluble in water and is administered orally. Following oral administration, it is well absorbed and achieves therapeutic concentrations in plasma and target tissues. As a fluoroquinolone, it distributes widely into body fluids and tissues, including the lungs, which is relevant for treating respiratory infections. The compound is metabolized in the liver and eliminated primarily via renal excretion. Its pharmacokinetic profile supports once-daily dosing in veterinary applications. The formulation for in vivo administration typically involves solubilizing the compound in suitable vehicles such as DMSO, Tween 80, and saline.
|
| Toxicity/Toxicokinetics |
Danofloxacin has a well-established safety profile in veterinary species. As a fluoroquinolone antibiotic, it may cause adverse effects such as gastrointestinal disturbances, central nervous system effects, and cartilage damage in juvenile animals, which are class effects of this drug class. It is contraindicated in animals with known hypersensitivity to fluoroquinolones. The safety margin is generally favorable when used at recommended therapeutic doses. In toxicity studies, the compound has demonstrated acceptable safety profiles in target species. However, as with all fluoroquinolones, caution should be exercised in young, growing animals due to the potential for arthropathy.
|
| References | |
| Additional Infomation |
Danofloxacin belongs to the quinolone class of drugs. Danofloxacin is a fluoroquinolone antibiotic used in veterinary medicine. See also: Danofloxacin mesylate (in salt form).
Danofloxacin (CAS# 112398-08-0) is a third-generation fluoroquinolone antibiotic used exclusively in veterinary medicine. It was developed by Pfizer and introduced in 1991 as a synthetic analog of ciprofloxacin. The compound is also known by the developmental code CP-76136-27. It is indicated for the treatment of respiratory diseases in cattle, pigs, and chickens. Danofloxacin functions by inhibiting bacterial DNA gyrase, thereby preventing DNA replication. The free base form is slightly soluble in water and is available as a research-grade compound. It is not approved for human use and is strictly limited to veterinary applications. |
| Molecular Formula |
C19H20FN3O3
|
|---|---|
| Molecular Weight |
357.37900
|
| Exact Mass |
357.148
|
| Elemental Analysis |
C, 63.86; H, 5.64; F, 5.32; N, 11.76; O, 13.43
|
| CAS # |
112398-08-0
|
| Related CAS # |
Danofloxacin mesylate;119478-55-6;Danofloxacin-d3;1825377-28-3
|
| PubChem CID |
71335
|
| Appearance |
Solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
569.3±50.0 °C at 760 mmHg
|
| Melting Point |
268-272ºC
|
| Flash Point |
298.1±30.1 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.679
|
| LogP |
1.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
|
| Complexity |
679
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CN1C[C@@H]2C[C@H]1CN2C3=C(C=C4C(=C3)N(C=C(C4=O)C(=O)O)C5CC5)F
|
| InChi Key |
QMLVECGLEOSESV-RYUDHWBXSA-N
|
| InChi Code |
InChI=1S/C19H20FN3O3/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/h5-6,9-12H,2-4,7-8H2,1H3,(H,25,26)/t11-,12-/m0/s1
|
| Chemical Name |
1-Cyclopropyl-6-fluoro-7-[(1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl]-4-oxoquinoline-3-carboxylic acid
|
| Synonyms |
Danofloxacine; Danofloxacin; Danofloxacino;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~4.59 mg/mL (~12.84 mM)
|
|---|---|
| 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 | 2.7981 mL | 13.9907 mL | 27.9814 mL | |
| 5 mM | 0.5596 mL | 2.7981 mL | 5.5963 mL | |
| 10 mM | 0.2798 mL | 1.3991 mL | 2.7981 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
