Pefloxacin mesylate dihydrate  (Synonyms: Pefloxacinium mesylate dihydrate)

Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC₅₀ of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC₉₀s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies^{[1][2][3][4][5][6][7][8][9]}.

Pefloxacin mesylate dihydrate 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 dihydrate 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.

Pefloxacin (cumulative total dose: 1.25-1280 mg/kg; s.c.; divided injection, every 6 h) mesylate dihydrate shows a high maximal antibacterial effect (E_max) against 15 gram-negative bacilli infections in a neutropenic mouse thigh infection model, and can reduce the bacterial load in infected mice^[4].
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.

465.49

C₁₈H₂₈FN₃O₈S

149676-40-4

Solid

White to off-white

O=C(C1=CN(CC)C2=C(C=C(F)C(N3CCN(C)CC3)=C2)C1=O)O.CS(=O)(O)=O.O.O

Room temperature in continental US; may vary elsewhere.

* 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. 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.

• [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]