Besifloxacin Hydrochloride  (Synonyms: 盐酸贝西沙星)

Besifloxacin Hydrochloride is a fourth generation fluoroquinolone antibiotic. Besifloxacin Hydrochloride is a DNA gyrase and topoisomerase IV inhibitor. Besifloxacin Hydrochloride has broad-spectrum antibacterial activity, it is effective against Gram-negative and Gram-positive aerobic and anaerobic strains and reduces the incidence of drug resistance. Besifloxacin Hydrochloride has anti-inflammatory activity. Besifloxacin Hydrochloride can be used in bacterial conjunctivitis research^[1][2][3][4].

Besifloxacin Hydrochloride (0.1-30 μg/mL, 18 h) 以剂量依赖性方式抑制 THP-1 单核细胞 IL-1α、G-CSF、IL-1ra、IL-6、GM-CSF、IL-12p40、IL-1β、IL-8、IP-10、MCP-1 和 MIP-1α细胞因子的表达^[1]。
Besifloxacin Hydrochloride 对金黄色葡萄球菌分离株累计最低抑菌浓度 (MIC) 值小，且 MIC 随着分离株耐药性的增加而增幅最小 (0.015-8 μg/mL)^[2]。
Besifloxacin Hydrochloride 的 MIC 随着金黄色葡萄球菌分离株的 DNA 促旋酶和拓扑异构酶 IV 中存在的喹诺酮耐药决定区 (QRDR) 突变数量的增加而增幅最小^[2]。

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

Besifloxacin Hydrochloride (6 mg/mL，局部给药，8小时内滴 19 次) 可降低兔耐甲氧西林金黄色葡萄球菌 (MRSA) 感染的临床严重程度^[4]。

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

430.30

盐酸贝西沙星

C₁₉H₂₂Cl₂FN₃O₃

405165-61-9

固体

White to off-white

盐酸贝西沙星

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Zhang JZ, et al. Besifloxacin, a novel fluoroquinolone antimicrobial agent, exhibits potent inhibition of pro-inflammatory cytokines in human THP-1 monocytes. J Antimicrob Chemother. 2008 Jan;61(1):111-6.  [Content Brief]

  [2]. Sanfilippo CM, et al. Topoisomerase mutations that are associated with high-level resistance to earlier fluoroquinolones in Staphylococcus aureus have less effect on the antibacterial activity of besifloxacin. Chemotherapy. 2011;57(5):363-71.  [Content Brief]

  [3]. Haas W, et al. Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria. Antimicrob Agents Chemother. 2009 Aug;53(8):3552-60.  [Content Brief]

  [4]. Sanders ME, et al. Efficacy of besifloxacin in an early treatment model of methicillin-resistant Staphylococcus aureus keratitis. J Ocul Pharmacol Ther. 2010 Apr;26(2):193-8.  [Content Brief]