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MedKoo Cat#: 318459 | Name: Pefloxacin Mesylate Dihydrate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pefloxacin mesylate dihydrate is a synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.

Chemical Structure

Pefloxacin Mesylate Dihydrate
Pefloxacin Mesylate Dihydrate
CAS#149676-40-4

Theoretical Analysis

MedKoo Cat#: 318459

Name: Pefloxacin Mesylate Dihydrate

CAS#: 149676-40-4

Chemical Formula: C18H28FN3O8S

Exact Mass:

Molecular Weight: 465.49

Elemental Analysis: C, 46.44; H, 6.06; F, 4.08; N, 9.03; O, 27.50; S, 6.89

Price and Availability

Size Price Availability Quantity
1g USD 150.00
2g USD 250.00
5g USD 450.00
10g USD 650.00
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Synonym
Pefloxacin Mesylate Dihydrate; Peflacine; UNII-CX28QC6FU0; Pefloxacin (mesylate dihydrate); Peflacin;
IUPAC/Chemical Name
1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid;methanesulfonic acid;dihydrate
InChi Key
LEULAXMUNMRLPW-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H20FN3O3.CH4O3S.2H2O/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);2*1H2
SMILES Code
CCN1C=C(C(=O)C2=CC(=C(C=C21)N3CCN(CC3)C)F)C(=O)O.CS(=O)(=O)O.O.O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pefloxacin mesylate dehydrate is an antibacterial agent and prevents bacterial DNA replication by inhibiting DNA gyrase (topoisomerse).
In vitro activity:
PFLX (pefloxacin) was photodegraded in 5h and forms photoproduct under UVA exposure. At the non photocytotoxic dose PFLX, shows reduced phagocytosis activity, NO (nitric oxide) production, large vacuole formation and down regulated IL-6, TNF-α and IL-1 in BALB/c macrophages at both genes and proteins levels. At higher doses (photocytotoxic doses), PFLX induced a concentration dependent decrease in cell viability of human keratinocyte cell line (HaCaT) and peritoneal macrophages of BALB/c mice. Reference: J Photochem Photobiol B. 2018 Jan;178:593-605. https://pubmed.ncbi.nlm.nih.gov/29275239/
In vivo activity:
The aim of this study was to investigate the changes in the number of serotonergic immunoreactive fibers and mast cells after pefloxacin treatment in the parotid and sublingual glands of rats to detect the possible neurotoxic effect of pefloxacin. These results suggest that pefloxacin treatment can modify the finely controlled communication between the immune- and the peripheral nervous systems, resulting neurogenic inflammatory process. Reference: Drug Chem Toxicol. 2020 Sep;43(5):496-503. https://pubmed.ncbi.nlm.nih.gov/30257570/
Solvent mg/mL mM
Solubility
DMF 3.0 6.44
DMSO 7.0 15.04
DMSO:PBS (pH 7.2) (1:3) 0.3 0.54
Water 67.0 143.93
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 465.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Singh J, Srivastva AK, Mandal P, Chandra S, Dubey D, Dwivedi A, Chopra D, Tripathi A, Ray RS. Under ambient UVA exposure, pefloxacin exhibits both immunomodulatory and genotoxic effects via multiple mechanisms. J Photochem Photobiol B. 2018 Jan;178:593-605. doi: 10.1016/j.jphotobiol.2017.12.014. Epub 2017 Dec 15. PMID: 29275239. 2. Puc J, Kwiatkowski P, Pacanowski J, Rotbart-Fiedor M, Wardawa A, Mazurek AP, Rowinski W, Hardy MA, Fiedor P. Mitochondrial activity after cold preservation of pancreatic islet cells treated with pefloxacin (PFX). Ann Transplant. 1998;3(1):38-41. PMID: 9869897. 3. Skopkó BE, Deák Á, Matesz C, Kelentey B, Bácskai T. Pefloxacin induced changes in serotonergic innervation and mast cell number in rat salivary glands. Drug Chem Toxicol. 2020 Sep;43(5):496-503. doi: 10.1080/01480545.2018.1508217. Epub 2018 Sep 27. PMID: 30257570.
In vitro protocol:
1. Singh J, Srivastva AK, Mandal P, Chandra S, Dubey D, Dwivedi A, Chopra D, Tripathi A, Ray RS. Under ambient UVA exposure, pefloxacin exhibits both immunomodulatory and genotoxic effects via multiple mechanisms. J Photochem Photobiol B. 2018 Jan;178:593-605. doi: 10.1016/j.jphotobiol.2017.12.014. Epub 2017 Dec 15. PMID: 29275239. 2. Puc J, Kwiatkowski P, Pacanowski J, Rotbart-Fiedor M, Wardawa A, Mazurek AP, Rowinski W, Hardy MA, Fiedor P. Mitochondrial activity after cold preservation of pancreatic islet cells treated with pefloxacin (PFX). Ann Transplant. 1998;3(1):38-41. PMID: 9869897.
In vivo protocol:
1. Skopkó BE, Deák Á, Matesz C, Kelentey B, Bácskai T. Pefloxacin induced changes in serotonergic innervation and mast cell number in rat salivary glands. Drug Chem Toxicol. 2020 Sep;43(5):496-503. doi: 10.1080/01480545.2018.1508217. Epub 2018 Sep 27. PMID: 30257570.
1: Li A, Song Z. Study of silver nanoparticles sensitized fluorescence and second-order scattering of terbium(III)-pefloxacin mesylate complex and determination of pefloxacin mesylate. ScientificWorldJournal. 2014;2014:742935. doi: 10.1155/2014/742935. Epub 2014 May 6. PubMed PMID: 24892083; PubMed Central PMCID: PMC4032712. 2: Guo M, Lu XW, Ran XY, Hu RH. [Molecular transport mechanism of pefloxacin mesylate binding with transferrin]. Yao Xue Xue Bao. 2012 Nov;47(11):1503-10. Chinese. PubMed PMID: 23387084. 3: Liu Y, Huang Y, Liu J, Wang W, Liu G, Zhao R. 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. J Chromatogr A. 2012 Jul 13;1246:15-21. doi: 10.1016/j.chroma.2012.01.045. Epub 2012 Jan 25. PubMed PMID: 22321951. 4: Liu R, Li N, Liu N, Zhou X, Dong ZM, Wen XJ, Liu LC. Effects of systemic ornidazole, systemic and local compound ornidazole and pefloxacin mesylate on experimental periodontitis in rats. Med Sci Monit. 2012 Mar;18(3):BR95-102. PubMed PMID: 22367122; PubMed Central PMCID: PMC3560749. 5: Xie Y, Song Y, Zhang Y, Zhao B. Near-infrared spectroscopy quantitative determination of pefloxacin mesylate concentration in pharmaceuticals by using partial least squares and principal component regression multivariate calibration. Spectrochim Acta A Mol Biomol Spectrosc. 2010 May;75(5):1535-9. doi: 10.1016/j.saa.2010.02.012. Epub 2010 Feb 21. PubMed PMID: 20299275. 6: Deng B, Li L, Shi A, Kang Y. Pharmacokinetics of pefloxacin mesylate in human urine using capillary electrophoresis electrochemiluminescence detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Aug 15;877(24):2585-8. doi: 10.1016/j.jchromb.2009.06.021. Epub 2009 Jun 21. PubMed PMID: 19576860. 7: Basavaiah K, Prameela HC, Somashekar BC. Spectrophotometric determination of pefloxacin mesylate in pharmaceuticals. Acta Pharm. 2007 Jun;57(2):221-30. PubMed PMID: 17507318. 8: Fan JC, Chen X, Wang Y, Fan CP, Shang ZC. Binding interactions of pefloxacin mesylate with bovine lactoferrin and human serum albumin. J Zhejiang Univ Sci B. 2006 Jun;7(6):452-8. PubMed PMID: 16691639; PubMed Central PMCID: PMC1473993. 9: Sultana Y, Aqil M, Ali A. Ion-activated, Gelrite-based in situ ophthalmic gels of pefloxacin mesylate: comparison with conventional eye drops. Drug Deliv. 2006 May-Jun;13(3):215-9. PubMed PMID: 16556574. 10: Sultana Y, Aqil M, Ali A. Ocular inserts for controlled delivery of pefloxacin mesylate: preparation and evaluation. Acta Pharm. 2005 Sep;55(3):305-14. PubMed PMID: 16375841. 11: Bharath S, Hiremath SR. Ocular delivery systems of pefloxacin mesylate. Pharmazie. 1999 Jan;54(1):55-8. PubMed PMID: 9987797. 12: Isaacs RD, Ellis-Pegler RB. Successful treatment of Morganella morganii meningitis with pefloxacin mesylate. J Antimicrob Chemother. 1987 Nov;20(5):769-70. PubMed PMID: 3480886. 13: Montay G, Goueffon Y, Roquet F. Absorption, distribution, metabolic fate, and elimination of pefloxacin mesylate in mice, rats, dogs, monkeys, and humans. Antimicrob Agents Chemother. 1984 Apr;25(4):463-72. PubMed PMID: 6587830; PubMed Central PMCID: PMC185553. 14: Sultana Y, Aqil M, Ali A, Zafar S. Evaluation of carbopol-methyl cellulose based sustained-release ocular delivery system for pefloxacin mesylate using rabbit eye model. Pharm Dev Technol. 2006;11(3):313-9. PubMed PMID: 16895842. 15: Chao JB, Tong HB, Liu DS, Huang SP. Preparation and characterization of inclusion complexes of pefloxacin mesylate with three kinds of cyclodextrins. Spectrochim Acta A Mol Biomol Spectrosc. 2006 May 1;64(1):166-70. Epub 2005 Aug 10. PubMed PMID: 16098803. 16: Sultana Y, Jha MC, Ali A, Aqil M. A three-way comparative study on the efficacy of twin sol to gel systems and marketed eye drops of pefloxacin mesylate. J Ocul Pharmacol Ther. 2004 Aug;20(4):363-71. PubMed PMID: 15321031. 17: Pozdniakova VP, Nestetrova LIa, Smirnova LB, Iakovlev VP, Blatun LA, Koshil' OI, Fedorov SM, Bakalova LA, Strachunskiĭ LS, Kurmanova KB. [Pefloxacin mesylate--clinical effectiveness in various forms of infectious-inflammatory diseases]. Antibiot Khimioter. 1997;42(7):20-3. Russian. PubMed PMID: 9334143. 18: Rose TF, Ellis-Pegler R, Collins J, Small M. Oral pefloxacin mesylate in the treatment of continuous ambulatory peritoneal dialysis associated peritonitis: an open non-comparative study. J Antimicrob Chemother. 1990 May;25(5):853-9. PubMed PMID: 2373667.