| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g | |||
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| Targets |
Quinolone
Pefloxacin mesylate targets bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, which are essential enzymes for bacterial DNA replication, transcription, repair, and recombination. By inhibiting these enzymes, it prevents the supercoiling and uncoiling of bacterial DNA, leading to the arrest of DNA synthesis and cell death. Its potent activity against a broad range of bacteria, including MRSA, is attributed to its high affinity for these targets. The compound's IC₅₀ of 6.7 nM reflects its high potency. |
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| ln Vitro |
In vitro, Pefloxacin mesylate exhibits potent antibacterial activity against a broad range of Gram-negative and Gram-positive bacteria. Its activity is measured by determining the minimum inhibitory concentration (MIC) against various bacterial strains. It is effective against methicillin-resistant S. aureus (MRSA). Its potency, with an IC₅₀ of 6.7 nM, makes it a highly effective antibacterial agent. The compound is used in microbiological research to study bacterial resistance mechanisms.
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| ln Vivo |
In vivo, Pefloxacin mesylate is used to treat infections due to susceptible organisms. It is effective against a variety of infections, including those of the respiratory tract, urinary tract, and skin. Its broad-spectrum activity and good tissue penetration make it useful for treating systemic infections. The compound is administered orally or intravenously. Its clinical use is limited by the development of bacterial resistance and potential side effects.
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| Enzyme Assay |
In vitro non-cell enzyme assays for Pefloxacin mesylate involve measuring its inhibition of DNA gyrase and topoisomerase IV. Purified enzymes are incubated with the compound, a DNA substrate, and ATP. The inhibition of DNA supercoiling or relaxation is measured by gel electrophoresis or fluorescence-based assays. IC₅₀ values, such as the 6.7 nM for its antibacterial activity, are determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for Pefloxacin mesylate use standard microbiological methods, such as broth microdilution and agar diffusion, to determine the MIC against various bacterial strains. Time-kill assays are used to evaluate its bactericidal activity over time. Its activity against MRSA is of particular interest. Cytotoxicity assays using mammalian cell lines are performed to assess its selectivity.
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| Animal Protocol |
In vivo animal studies for Pefloxacin mesylate employ models of bacterial infection, such as murine sepsis or pneumonia models. The compound is administered, and its efficacy is measured by the reduction in bacterial load, survival rates, or clinical signs of infection. Pharmacokinetic studies are also performed to characterize its absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
Pefloxacin mesylate has a molecular weight of 429.46 g/mol and a molecular formula of C₁₈H₂₄FN₃O₆S. It is a white to off-white powder. It is soluble in water. The compound should be stored at room temperature, protected from light and moisture. Its stability is good under normal storage conditions.
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| Toxicity/Toxicokinetics |
Pefloxacin mesylate, like other fluoroquinolones, can cause side effects such as gastrointestinal disturbances, central nervous system effects (dizziness, headache), and tendonitis. It is contraindicated in patients with a history of hypersensitivity to quinolones. Its use in children and adolescents is limited due to the risk of cartilage damage. The compound is not intended for human therapeutic use without a prescription.
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| References | |
| Additional Infomation |
A synthetic broad-spectrum fluoroquinolone antibacterial agent effective against most Gram-negative and Gram-positive bacteria.
See also: Pefigstigmine (note moved to). Pefloxacin mesylate is a broad-spectrum, third-generation fluoroquinolone antibacterial agent. It is effective against a variety of organisms, including MRSA. It has an IC₅₀ of 6.7 nM. It is used to treat infections caused by susceptible bacteria. It is not approved for clinical use in all countries. |
| Molecular Formula |
C17H20FN3O3.CH4O3S
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|---|---|
| Molecular Weight |
429.46
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| Exact Mass |
429.136
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| Elemental Analysis |
C, 50.34; H, 5.63; F, 4.42; N, 9.78; O, 22.35; S, 7.47
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| CAS # |
70458-95-6
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| Related CAS # |
Pefloxacin;70458-92-3;Pefloxacin mesylate dihydrate;149676-40-4
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| PubChem CID |
119525
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| Appearance |
Solid powder
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| Density |
1.32 g/cm3
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| Boiling Point |
529.1ºC at 760 mmHg
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| Flash Point |
273.8ºC
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| LogP |
2.198
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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 |
29
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| Complexity |
638
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
HQQSBEDKMRHYME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H20FN3O3.CH4O3S/c1-3-20-10-12(17(23)24)16(22)11-8-13(18)15(9-14(11)20)21-6-4-19(2)5-7-21;1-5(2,3)4/h8-10H,3-7H2,1-2H3,(H,23,24);1H3,(H,2,3,4)
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| Chemical Name |
3-Quinolinecarboxylic acid, 1,4-dihydro-1-ethyl-6-fluoro-7-(4-methyl-1-piperazinyl)-4-oxo-, mesylate
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| Synonyms |
Pefloxacin; 1584RB; 1589 RB; EU 5306; EU-5306; Pefloxacin mesylate
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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) |
H2O : ≥ 100 mg/mL (~232.85 mM)
DMSO : ~12.5 mg/mL (~29.11 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.91 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 12.5 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: ≥ 1.25 mg/mL (2.91 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 12.5 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: ≥ 1.25 mg/mL (2.91 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: 150 mg/mL (349.28 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 | 2.3285 mL | 11.6425 mL | 23.2851 mL | |
| 5 mM | 0.4657 mL | 2.3285 mL | 4.6570 mL | |
| 10 mM | 0.2329 mL | 1.1643 mL | 2.3285 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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