| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Quinolone
Bacterial DNA gyrase and DNA topoisomerase IV. Finafloxacin selectively targets bacterial type II topoisomerases. |
|---|---|
| ln Vitro |
In vitro, Finafloxacin shows potent antibacterial activity that is enhanced in acidic environments (pH 5.0-6.0). It selectively targets bacterial type II topoisomerases, including DNA gyrase and topoisomerase IV. The compound's unique property of maintaining antimicrobial activity in acidic conditions allows for improved efficacy and penetration into infected tissues. Finafloxacin is effective against various bacterial pathogens causing urinary tract infections and skin and soft tissue infections.
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| ln Vivo |
In vivo, Finafloxacin was approved by the FDA in 2014 for treating swimmer's ear (acute otitis externa). Its mechanism of action involves the inhibition of bacterial type II topoisomerase enzymes. The compound's enhanced activity in acidic environments makes it particularly effective for infections where tissue pH is reduced. Finafloxacin is also being studied for urinary tract infections and bacterial skin and soft tissue infections.
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| Enzyme Assay |
Non-cell enzyme assays are performed using purified bacterial DNA gyrase and topoisomerase IV enzymes. Supercoiling and decatenation assays are used to measure enzyme activity. DNA gyrase-mediated supercoiling of relaxed plasmid DNA is measured in the presence of ATP and varying concentrations of Finafloxacin (0.001-100 μM). Topoisomerase IV-mediated decatenation of kinetoplast DNA is measured similarly. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular antibacterial assays are performed using standard broth microdilution methods according to CLSI guidelines. Bacterial cultures are grown to mid-log phase and diluted to ~5×10⁵ CFU/mL. Two-fold serial dilutions of Finafloxacin (0.001-128 μg/mL) are prepared in 96-well plates at pH 5.0-6.0 and pH 7.4 to assess pH-dependent activity. Bacteria are added and incubated at 37°C for 18-24 hours. The MIC is determined as the lowest concentration with no visible growth. MBC is determined by subculturing onto agar plates.
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| Animal Protocol |
In vivo efficacy studies are conducted in animal models of infection, including acute otitis externa (swimmer's ear), urinary tract infections, and skin and soft tissue infections. Finafloxacin is administered topically, orally, or intravenously at doses determined from pharmacokinetic studies. Efficacy endpoints include bacterial load (CFU/g tissue), clinical cure rates, and histopathological analysis. The compound's enhanced activity at acidic pH is evaluated in models where tissue acidosis is present.
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| ADME/Pharmacokinetics |
Finafloxacin is a fluoroquinolone antibiotic with favorable pharmacokinetic properties. It is approved for topical use in acute otitis externa. The compound has a molecular weight of 398.39 and a molecular formula appropriate for its class. It shows good tissue penetration and is effective in acidic environments. Further pharmacokinetic parameters are available in the product labeling.
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| Toxicity/Toxicokinetics |
Finafloxacin is generally well tolerated as a topical preparation. As a fluoroquinolone, systemic use may be associated with tendonitis, tendon rupture, peripheral neuropathy, and central nervous system effects. No significant local toxicity has been reported at therapeutic concentrations. The compound is contraindicated in patients with known hypersensitivity to fluoroquinolones.
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| References |
[1]. Finafloxacin: first global approval. Drugs. 2015 Apr;75(6):687-93. [2]. Finafloxacin for the treatment of urinary tract infections. Expert Opin Investig Drugs. 2015;24(7):957-63. |
| Additional Infomation |
Fenafloxacin is a quinolone antibiotic with the chemical name 4-oxo-1,4-dihydroquinoline-3-carboxylic acid, in which the 1, 6, 7, and 8 positions are substituted with cyclopropyl, fluorine, hexahydropyrrolo[3,4-b][1,4]oxazin-6-yl, and cyano groups, respectively. It is an antibiotic used to treat acute otitis externa (swimmer's ear) caused by Pseudomonas aeruginosa and Staphylococcus aureus. It has antibacterial activity. It is a quinolone compound, a monocarboxylic acid compound, an organofluorine compound, a secondary amino compound, a tertiary amino compound, a nitrile compound, and also a cyclopropane compound. Fenafloxacin is a fluoroquinolone antibiotic indicated for the treatment of acute otitis externa (swimmer's ear) caused by Pseudomonas aeruginosa and Staphylococcus aureus. Fenafloxacin is marketed by Novartis under the brand name Xtoro™ and was approved by the FDA in December 2014. Fenafloxacin is a quinolone antibacterial drug.
Indications Fenafloxacin is indicated for the treatment of acute otitis externa (AOE) caused by fennafloxacin-sensitive Pseudomonas aeruginosa and Staphylococcus aureus, with or without earplugs. Suitable for patients 1 year of age and older. FDA Label Mechanism of Action Fenafloxacin is a fluoroquinolone antibiotic that selectively inhibits bacterial type II topoisomerase, DNA gyrase, and topoisomerase IV, enzymes essential for bacterial DNA replication, transcription, repair, and recombination. Finafloxacin (Xtoro) is a fluoroquinolone antibiotic approved by the FDA in 2014 for treating acute otitis externa (swimmer's ear). It belongs to a new 8-cyano subclass of fluoroquinolones. Its unique property of maintaining antimicrobial activity in acidic conditions (pH 5.0-6.0) allows for improved efficacy in infected tissues. The compound is also being studied for urinary tract infections and skin and soft tissue infections. |
| Molecular Formula |
C20H19N4O4F.HCL
|
|---|---|
| Molecular Weight |
434.8486
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| Exact Mass |
398.139
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| Elemental Analysis |
C, 60.30; H, 4.81; F, 4.77; N, 14.06; O, 16.06
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| CAS # |
209342-40-5
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| Related CAS # |
Finafloxacin hydrochloride;209342-41-6
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| PubChem CID |
11567473
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| Appearance |
Solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
686.2±55.0 °C at 760 mmHg
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| Flash Point |
368.8±31.5 °C
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| Vapour Pressure |
0.0±2.2 mmHg at 25°C
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| Index of Refraction |
1.700
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| LogP |
-0.85
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
806
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4C[C@]5([H])OCCN[C@@]5([H])C4)=C3C#N)C1=O)O
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| InChi Key |
FYMHQCNFKNMJAV-HOTGVXAUSA-N
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| InChi Code |
InChI=1S/C20H19FN4O4/c21-14-5-11-17(25(10-1-2-10)7-13(19(11)26)20(27)28)12(6-22)18(14)24-8-15-16(9-24)29-4-3-23-15/h5,7,10,15-16,23H,1-4,8-9H2,(H,27,28)/t15-,16-/m0/s1
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| Chemical Name |
8-Cyano-1-cyclopropyl-6-fluoro-7-[(4aS,7aS)-hexahydropyrrolo[3,4-b][1,4]oxazin-6(2H)-yl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
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| Synonyms |
Finafloxacin;brand name Xtoro.
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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 |
| 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) |
DMSO : ~6.4 mg/mL (~16.06 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 | 2.2996 mL | 11.4982 mL | 22.9964 mL | |
| 5 mM | 0.4599 mL | 2.2996 mL | 4.5993 mL | |
| 10 mM | 0.2300 mL | 1.1498 mL | 2.2996 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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