Clinafloxacin  (Synonyms: 克林沙星; AM-1091; CI-960; PD 127391)

Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro^[1]. Clinafloxacin is against DNA gyrase and topoisomerase IV of?S. aureus with IC₅₀ values of 0.92 μg/ml and 1.62 μg/ml, respectively^[2].

Clinafloxacin 表现出抗 S. pneumonia 的活性，parC-gyrA突变体的MIC为1μg/mL的肺炎^[2]。
盐酸克林沙星对靶向改变的突变体具有抗菌活性 S. aureus。它对抗野生型 S. aureus, gyr A mutant S. aureus 和 gyrA mutant S. aureus 的 MIC 值分别为 0.016 μg/mL、0.063 μg/mL和 0.915 μg/mL^[3]。

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

克林沙星对青霉素耐药、环丙沙星敏感的肺炎球菌性脑膜炎在家兔模型中的处理非常有效。
与CS菌株 (2349) (克林沙星MIC=0.12 μg/mL)，剂量为10 mg/ kg 和 20 mg/kg 每天克林沙星在 6 小时达到初始减少。两者此时均具有杀菌作用，但在 24 小时后出现再生，24 小时时平均 log cfu/mL 的最终减少分别为 22.30 和 23.83。然而，对于 CR 菌株 (4371) (克林沙星 MIC=0.5 μg/mL)，即使每天 20 mg/kg 克林沙星在脑膜炎兔模型中的任何时间点都不会降低细菌滴度^[3]。

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

365.79

C₁₇H₁₇ClFN₃O₃

105956-97-6

固体

White to yellow

克林沙星

Room temperature in continental US; may vary elsewhere.

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• [1]. M Takei, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition.Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.  [Content Brief]

  [2]. Randa H Abdelkreem, et al. DNA Gyrase and Topoisomerase IV Mutations and their effect on Quinolones Resistant Proteus mirabilis among UTIs Patients. Pak J Med Sci. Sep-Oct 2020;36(6):1234-1240.  [Content Brief]

  [3]. A Domenech, et al. Experimental study of clinafloxacin alone and in combination in the treatment of ciprofloxacin-susceptible and -resistant pneumococcal meningitis.Microb Drug Resist. 2003;9 Suppl 1:S53-9.  [Content Brief]