Pefloxacin mesylate dihydrate  (Synonyms: 甲磺酸培氟沙星二水合物; 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 浓度在 ≤0.5 mg/L 时，可抑制 90% 的大肠杆菌和肺炎克雷伯菌等菌株；在浓度 4 mg/L时，可抑制 90% 的铜绿假单胞菌；浓度 16 mg/L 时，可抑制 90% 的脆弱拟杆菌^[1]。
Pefloxacin (0.06-64 mg/L) mesylate dihydrate 对葡萄球菌和大肠杆菌等多种细菌表现出良好的活性，但对阴道加德纳菌和Mobiluncus spp. 等细菌的活性较差^[2]。
Pefloxacin (5-60 μg/mL；30 min) 可抑制大肠杆菌拓扑异构酶 I 催化的 DNA 松弛反应，IC₅₀ 为 45 μg/mL^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Pefloxacin (累计总剂量：1.25-1280 mg/kg；皮下注射；分次注射，每 6 h 一次) mesylate dihydrate 在中性粒细胞减少小鼠大腿感染模型中，对 15 种革兰氏阴性杆菌感染表现出较高的最大抗菌效果 (E_max)，并可降低感染小鼠的细菌负荷^[4]。
Pefloxacin (200 mg/kg；皮下注射；UVA 照射前 2 h和照射后 5 h) mesylate dihydrate 可增加 UVA 引起的背部皮肤肿胀、晒伤细胞数量，减少表皮朗格汉斯细胞数量，并抑制小鼠局部接触性超敏反应^[5]。
Pefloxacin (每日最高 150 mg/kg；口服) 在小鼠中对结核分枝杆菌感染无效^[6]。
Pefloxacin (40-240 mg/kg；皮下注射；每 8-12 h 一次；3 天) 可显著降低感染约氏疟原虫的 Swiss albino小鼠的寄生虫血症并提高存活率，其疗效优于 Ciprofloxacin (HY-B0356)^[7]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

465.49

C₁₈H₂₈FN₃O₈S

149676-40-4

甲磺酸培氟沙星二水合物

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]