Finafloxacin
Based on 1 publication(s) in Google Scholar
Finafloxacin is an orally active fluoroquinolone antibacterial agent. Finafloxacin exerts broad-spectrum antibacterial activity by promoting DNA cleavage in the gyrase/topoisomerase IV (Topoisomerase IV) complex and inhibiting DNA synthesis. Finafloxacin is a weak substrate of NorA/Lde, can be effluxed by BpeAB-OprB/BpeEF-OprC, and can overcome BpeEF-OprC-mediated fluoroquinolone resistance, while also accumulating in macrophages and exhibiting intracellular bactericidal activity. Finafloxacin can be used for research on intracellular bacterial infections, melioidosis, tularemia, plague, acute otitis externa, complicated urinary tract infections, and pyelonephritis.
For research use only. We do not sell to patients.
- Purity : 98.75%
- CAS No.: 209342-40-5
- Formula: C20H19FN4O4
- Molecular Weight:398.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Finafloxacin
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Biological Activity
Description
IC50 & Target
[5]|
topoisomerase IV |
In Vitro
Finafloxacin (100 mg/L; 30 min) shows increased uptake and a lower MIC in S. aureus ATCC 25923 at pH 5.5 than at pH 7.4[1].
Finafloxacin (20 h) inhibits Burkholderia pseudomallei 1026b with an MIC of 0.125 mg/L at pH 5.8 and an MIC of 0.25 mg/L at pH 7.2, and retains activity against the BpeEF-OprC-expressing strain Bp282 at both pH values with an MIC of 2 mg/L[2].
Finafloxacin (16 μg/mL; 24 h) exerts bactericidal activity against both B. pseudomallei K96243 and 576 at pH 5 and pH 7 within 24 h, with enhanced killing at pH 5, and no recoverable bacteria for K96243 at 24 h[5].
Finafloxacin (100× MIC; 24 h) reduces B. pseudomallei persister cells, with no recoverable persister cells for strain 576 at pH 5 and for strain K96243 at pH 7[5].
Finafloxacin produces a > 4 log10 CFU reduction of intracellular L. monocytogenes in THP-1 cells at neutral pH, and an Emax of -2.7 log10 CFU against L. pneumophila[1].
Finafloxacin (1×-4× MIC; 24 h) reduces B. pseudomallei strain AI within J774 mouse macrophages at 1× and 4× MIC within 24 h[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUCinf |
|---|---|---|---|---|---|
| Mice[5] | 37.5 mg/kg | p.o. | 1.89 h | 7.24 μg/mL | 11.12 μg·h/mL |
In Vivo
Finafloxacin (23.1 mg/kg; p.o.; once every 8 hours; dosing initiated at 24 or 38 hours post-challenge and continued for 3 or 7 days) is effective against inhalational plague in BALB/c mice, with the 3-day regimen initiated at 24 or 38 hours producing 100% survival and the 7-day regimen initiated at 24/38 hours producing 100%/90% survival[3].
Finafloxacin (37.5 mg/kg; p.o.; once every 8 hours; 14 days) protects BALB/c mice against inhalational B. pseudomallei infection, producing 80% and 60% survival at day 63 when administration begins at 6 and 24 hours post-challenge, respectively, and promotes bacterial clearance in the spleen, liver, and lungs[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 8-10 weeks old)[3]
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Dosage:23.1 mg/kg
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Administration:p.o.; every 8 h; 3/7 days starting 24 h postchallenge; p.o.; every 8 h; 3/7 days starting 72 h postchallenge
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Result:At 24 h postchallenge, both the 3-day and 7-day regimens produced 100% survival to day 34/35.
At 72 h postchallenge, the 3-day regimen resulted in 0% survival, with all mice succumbing by day 16; disease scores resolved by day 7 and signs reappeared by day 11.
The 7-day regimen initiated at 72 h produced 50% survival; mice were completely protected until day 21 postchallenge, and survivors had no detectable colonizing bacteria or F. tularensis-typical histopathology.
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Animal Model:BALB/c (female, 8-10 weeks old)[3]
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Dosage:23.1 mg/kg
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Administration:p.o.; every 8 h; 3/7 days starting 24 h postchallenge; p.o.; every 8 h; 3/7 days starting 38 h postchallenge
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Result:At 24 h postchallenge, both the 3-day and 7-day regimens produced 100% survival at study end.
At 38 h postchallenge, the 3-day regimen produced 100% survival and the 7-day regimen produced 90% survival.
The 3-day regimen started at 38 h cleared active infection, although one mouse had chronic lesions.
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Animal Model:BALB/c (female, 8-10 weeks)[5]
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Dosage:37.5 mg/kg
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Administration:p.o.; every 8 h; for 14 days
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Result:Day 63 survival was 80% when administration was initiated at 6 h postchallenge and 60% when initiated at 24 h postchallenge.
When administration was initiated at 6 h, no bacteria were detected in the spleens or livers at 24 h after administration onset, and no B. pseudomallei was recovered from the remaining spleen or liver homogenates.
At cessation of 14-day administration initiated at 6 h, no recoverable bacteria were detected in the spleens, livers, or lungs, and remaining organ homogenates were negative.
When administration was initiated at 24 h, no recoverable bacteria were detected in the spleens, livers, or lungs at cessation of administration, and remaining organ homogenates were negative.
At day 63, among eight surviving mice started at 6 h, one mouse had B. pseudomallei in the spleen, liver, and lungs, and one other mouse had detectable bacteria in the lungs after incubation; 75% of these mice were not colonized in the spleen, liver, and lungs.
Among six surviving mice started at 24 h, one mouse was colonized, one other mouse had B. pseudomallei recovered from spleen homogenate, and 66% were not colonized.
Relapse in animals was not observed until day 45 with 6-h initiation or day 40 with 24-h initiation.
Chemical Information
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CAS No. 209342-40-5
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Appearance Solid
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Molecular Weight 398.39
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Formula C20H19FN4O4
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Color Light yellow to yellow
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Microb Pathog
Antibiotic discovery against Piscirickettsia salmonis using a combined in silico and in vitro approach. [Abstract]2023 Jul:180:106122. PMID: 37094756
Solvent & Solubility
In Vitro:
DMSO : 6.4 mg/mL (16.06 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (296 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[3]. Barnes KB, et al. Finafloxacin Is an Effective Treatment for Inhalational Tularemia and Plague in Mouse Models of Infection. Antimicrob Agents Chemother. 2021;65(6):e02294-20. Published 2021 May 18. [Content Brief]
[4]. Daisuke Fukuda, et al. Bacterial DNA topoisomerase IV and DNA gyrase inhibitors: history of the quinolones, their clinical usage and potential alternatives for the future, Journal of Antimicrobial Chemotherapy, Volume 81, Issue 3, March 2026, dkag054. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5101 mL | 12.5505 mL | 25.1010 mL | 62.7526 mL |
| 5 mM | 0.5020 mL | 2.5101 mL | 5.0202 mL | 12.5505 mL | |
| 10 mM | 0.2510 mL | 1.2551 mL | 2.5101 mL | 6.2753 mL | |
| 15 mM | 0.1673 mL | 0.8367 mL | 1.6734 mL | 4.1835 mL |
Finafloxacin Related Classifications
HY-13451 Related Classifications
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