Pefloxacin mesylate
Based on 3 publication(s) in Google Scholar
Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies.
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- Pureté : 99.70%
- CAS No.: 70458-95-6
- Formule: C18H24FN3O6S
- Masse moléculaire:429.46
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Pefloxacin mesylate
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Activité biologique
Description
IC50 & Target
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Quinolone |
In Vitro
Pefloxacin mesylate inhibits 90% of strains such as Escherichia coli and Klebsiella pneumoniae at ≤0.5 mg/L, 90% of Pseudomonas aeruginosa at 4 mg/L, and 90% of the Bacteroides fragilis group at 16 mg/L[1].
Pefloxacin (0.06-64 mg/L) mesylate shows good activity against many bacteria such as staphylococci and E. coli, but poor activity against bacteria like Gardnerella vaginalis and Mobiluncus spp.[2].
Pefloxacin (5-60 μg/mL; 30 min) can inhibit the DNA relaxation reaction catalyzed by E. coli topoisomerase I, with an IC50 of 45 μg/mL[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pefloxacin (200 mg/kg; s.c.; 2 h before and 5 h after UVA irradiation) can increase UVA-induced back skin swelling, the number of sunburn cells, reduce the number of epidermal Langerhans cells, and inhibit local contact hypersensitivity in mice[5].
Pefloxacin (up to 150 mg/kg; p.o.; daily) is ineffective against Mycobacterium tuberculosis infection in mice[6].
Pefloxacin (40-240 mg/kg; s.c.; every 8-12 h; 3 days) can significantly reduce parasitemia and increase the survival rate of Swiss albino mice infected with Plasmodium yoelii, with superior efficacy to Ciprofloxacin (HY-B0356)[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 70458-95-6
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Appearance Solid
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Masse moléculaire 429.46
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Formule C18H24FN3O6S
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Color White to off-white
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SMILES
O=C(C1=CN(CC)C2=C(C=C(F)C(N3CCN(C)CC3)=C2)C1=O)O.CS(=O)(O)=O
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Synonyms
Pefloxacinium mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Food Chem X
Machine learning prioritization of antibiotic residues in aquatic foods reveals exposure-driven genotoxic risk mediated by BCL2. [Abstract]2026 Feb 8:34:103646. PMID: 41756597 -
Xenobiotica
Human total clearance values and volumes of distribution of typical human cytochrome P450 2C9/19 substrates predicted by single-species allometric scaling using pharmacokinetic data sets from common marmosets genotyped for P450 2C19. [Abstract]2021 Apr;51(4):479-493. PMID: 33455494 -
Chemosphere
Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]2019 Jun:225:378-387. PMID: 30884299
Solvant et solubilité
In Vitro:
H2O : ≥ 100 mg/mL (232.85 mM)
DMSO : 12.5 mg/mL (29.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.91 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.91 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 150 mg/mL (349.28 mM); Clear solution; Need ultrasonic
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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (280 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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Instruction de manipulation (2659 KB)
Références
[1]. Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. [Content Brief]
[2]. Hussy P, et al. Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts. Antimicrob Agents Chemother. 1986 Jun;29(6):1073-8. [Content Brief]
[3]. Clarke AM, et al. In-vitro activity of pefloxacin compared to enoxacin, norfloxacin, gentamicin and new beta-lactams. J Antimicrob Chemother. 1985 Jan;15(1):39-44. [Content Brief]
[4]. Jones BM, et al. Activity of pefloxacin and thirteen other antimicrobial agents in vitro against isolates from hospital and genitourinary infections. J Antimicrob Chemother. 1986 Jun;17(6):739-46. [Content Brief]
[5]. Tabary X, et al. Effect of DNA gyrase inhibitors pefloxacin, five other quinolones, novobiocin, and clorobiocin on Escherichia coli topoisomerase I. Antimicrob Agents Chemother. 1987 Dec;31(12):1925-8. [Content Brief]
[6]. Fantin B, et al. Correlation between in vitro and in vivo activity of antimicrobial agents against gram-negative bacilli in a murine infection model. Antimicrob Agents Chemother. 1991 Jul;35(7):1413-22. [Content Brief]
[7]. Sun YW, et al. Pefloxacin and ciprofloxacin increase UVA-induced edema and immune suppression. Photodermatol Photoimmunol Photomed. 2001 Aug;17(4):172-7. [Content Brief]
[8]. Truffot-Pernot C, et al. Activities of pefloxacin and ofloxacin against mycobacteria: in vitro and mouse experiments. Tubercle. 1991 Mar;72(1):57-64. [Content Brief]
[9]. Salmon D, et al. Activities of pefloxacin and ciprofloxacin against experimental malaria in mice. Antimicrob Agents Chemother. 1990 Dec;34(12):2327-30. [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, 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 |
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| DMSO / H2O | 1 mM | 2.3285 mL | 11.6425 mL | 23.2851 mL | 58.2126 mL |
| 5 mM | 0.4657 mL | 2.3285 mL | 4.6570 mL | 11.6425 mL | |
| 10 mM | 0.2329 mL | 1.1643 mL | 2.3285 mL | 5.8213 mL | |
| 15 mM | 0.1552 mL | 0.7762 mL | 1.5523 mL | 3.8808 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1643 mL | 2.9106 mL | |
| 25 mM | 0.0931 mL | 0.4657 mL | 0.9314 mL | 2.3285 mL | |
| H2O | 30 mM | 0.0776 mL | 0.3881 mL | 0.7762 mL | 1.9404 mL |
| 40 mM | 0.0582 mL | 0.2911 mL | 0.5821 mL | 1.4553 mL | |
| 50 mM | 0.0466 mL | 0.2329 mL | 0.4657 mL | 1.1643 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3881 mL | 0.9702 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7277 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2329 mL | 0.5821 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.
Pefloxacin mesylate Related Classifications
HY-B0147A Related Classifications
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