Pefloxacin Mesylate

CAS# 70458-95-6

Pefloxacin Mesylate

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Chemical structure

Pefloxacin Mesylate

3D structure

Chemical Properties of Pefloxacin Mesylate

Cas No. 70458-95-6 SDF Download SDF
PubChem ID 119525 Appearance Powder
Formula C18H24FN3O6S M.Wt 429.46
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Pefloxacinium mesylate
Solubility H2O : ≥ 100 mg/mL (232.85 mM)
DMSO : 12.5 mg/mL (29.11 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;methanesulfonic acid
SMILES CCN1C=C(C(O)=O)C(=O)c2cc(F)c(cc12)N3CCN(C)CC3.C[S](O)(=O)=O
Standard InChIKey HQQSBEDKMRHYME-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Pefloxacin Mesylate

DescriptionPefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections. Pefloxacin is commonly referred to as afluoroquinolone (or quinolone) drug and is a member of the fluoroquinolone class of antibacterials. It is an analog of norfloxacin. It is a synthetic fluoroquinolone, belonging to the 3rd generation of quinolones. Pefloxacin is extensively prescribed in France. Pefloxacin has not been approved for use in the United States. The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

References:
[1]. Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. [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.

Pefloxacin Mesylate Dilution Calculator

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Pefloxacin Mesylate Molarity Calculator

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Preparing Stock Solutions of Pefloxacin Mesylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3285 mL 11.6425 mL 23.2851 mL 46.5701 mL 58.2126 mL
5 mM 0.4657 mL 2.3285 mL 4.657 mL 9.314 mL 11.6425 mL
10 mM 0.2329 mL 1.1643 mL 2.3285 mL 4.657 mL 5.8213 mL
50 mM 0.0466 mL 0.2329 mL 0.4657 mL 0.9314 mL 1.1643 mL
100 mM 0.0233 mL 0.1164 mL 0.2329 mL 0.4657 mL 0.5821 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Pefloxacin Mesylate

Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse)

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References on Pefloxacin Mesylate

Study of silver nanoparticles sensitized fluorescence and second-order scattering of terbium(III)-pefloxacin mesylate complex and determination of pefloxacin mesylate.[Pubmed:24892083]

ScientificWorldJournal. 2014;2014:742935.

alpha-Keto acid of Pefloxacin Mesylate (PFLX) can form the complex with Terbium(III). The intramolecular energy from PFLX to Terbium(III) ion takes place when excited, and thus Terbium(III) excited state is formed and then emits the characteristic fluorescence of Terbium(III), locating at 490, 545, 580, and 620 nm. The second-order scattering (SOS) peak at 545 nm also appears for the complex with the exciting wavelength of 273 nm. When the silver nanoparticles are added to the system, the luminescence intensity at 545 nm greatly increased. So, with the adding of nanoparticles to the Terbium(III)-PFLX complex, not only is the intramolecular energy promoted but also the SOS intensity is enhanced. The experimental results show that it is the silver nanoparticles with certain size and certain concentration which can greatly enhance the fluorescence-SOS intensity, and the relative intensity at 545 nm is proportional to the amount of PFLX. Based on this phenomenon, a novel method for the determination of PFLX has been developed and applied to the determination of PFLX in capsule and serum samples.

Superparamagnetic surface molecularly imprinted nanoparticles for water-soluble pefloxacin mesylate prepared via surface initiated atom transfer radical polymerization and its application in egg sample analysis.[Pubmed:22321951]

J Chromatogr A. 2012 Jul 13;1246:15-21.

The novel superparamagnetic surface molecularly imprinted Fe(3)O(4)@MIP nanoparticles for water-soluble Pefloxacin Mesylate (PEF-M) were prepared via surface initiated atom transfer radical polymerization (si-ATRP). The binary mixture of methanol and water was selected as the polar solvents for fabricating PEF-M imprinted MIPs. The Fe(3)O(4)@MIP exhibited high saturation magnetization of 41.4 emu/g leading to the fast separation. The adsorption behaviors indicated that the Fe(3)O(4)@MIP nanoparticles possessed specific recognition and high affinity towards template PEF-M in aqueous media. Moreover, Fe(3)O(4)@MIP nanoparticles were directly used to selectively enrich PEF-M from egg samples. By RP-HPLC analysis, the recoveries of PEF-M were obtained as 92.8-96.5% with relative standard division of 2.4-4.0%.

[Molecular transport mechanism of pefloxacin mesylate binding with transferrin].[Pubmed:23387084]

Yao Xue Xue Bao. 2012 Nov;47(11):1503-10.

The binding mechanism between Pefloxacin Mesylate (PM) and transferrin (Tf) was explored using spectral experiment combined with molecular modeling techniques. The binding parameters and thermodynamic functions of PM-Tf solution system were measured at different temperatures. The effect of PM on molecular conformation of Tf was investigated and the interaction mechanism was also discussed. The results showed that dynamic quenching mechanism occurs with PM binding to Tf. The value of binding distances (r) is low, which indicates the occurrence of energy transfer. The drug had conformational effect on Tf, which resulted in changes of hydrophobic environment of the binding domain in Tf. According to the obtained thermodynamic parameters, the main interaction force between PM and Tf is attributed to hydrophobic bonding. The results of molecular modeling revealed that hydrophobic and hydrogen bonds are main binding forces in the PM-Tf system. These results were in accordance with spectral experiments. The research results have given a better theoretical reference for the study of pharmacological mechanism between protein and quinolone.

Effects of systemic ornidazole, systemic and local compound ornidazole and pefloxacin mesylate on experimental periodontitis in rats.[Pubmed:22367122]

Med Sci Monit. 2012 Mar;18(3):BR95-102.

BACKGROUND: The purpose of the current study is to evaluate the effects of systemic ornidazole (SO) and systemic and local compound ornidazole and Pefloxacin Mesylate (SCOPM/LCOMP) on the inflammatory response associated with rat experimental chronic periodontitis (ECP) in sites with subgingival debridement. MATERIAL/METHODS: Periodontitis was induced in male Sprague-Dawley rats by placing a thin steel ligature around the upper first molars and inoculating them with Porphyromonas gingivalis 381. After the successful induction of the rat ECP, the periodontitis rats were randomly divided into 3 different combined treatment groups: (A) SO with scaling and root planing (SRP); (B) SCOMP with SRP; and (C) LCOMP with SRP. After 2 weeks the effects of the treatments were evaluated based on gingivitis, plaque index, probing pocket depth, aspartate aminotransferase, alveolar bone loss, and hematoxylin-eosin staining of the region around the first molars. RESULTS: After treatment, comparison with ECP was performed. The mean percentage reductions of SBI in SO, SCOPM, and LCOPM were 27.73%, 33.61%, and 58.82%, respectively. Those of PI were 33.20%, 42.80%, and 60.00%; those of PPD were 48.66%, 55.70%, and 72.48%; those of GCF-AST were 41.64%, 49.03%, and 66.42%; and those of ABL were 41.19%, 43.63%, and 54.47%, respectively. The inflammatory score of H&E showed median scores of 2.5, 1.75, 1.63, and 0.95 for ECP, SO, SCOMP, and LCOMP, respectively. All 3 treatment groups exhibited significantly reduced inflammation indicators (P<0.05). Of the 3, group C was the most effective (P<0.05). CONCLUSIONS: Although all the combined treatment groups responded to therapy with significant resolution of the infection, adjunctive LCOMP therapy is more effective for periodontitis.

Description

Pefloxacin mesylate is a an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse) Target: DNA gyrase Pefloxacin is a synthetic chemotherapeutic agent used to treat severe and life-threatening bacterial infections.

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