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Gemifloxacin Mesylate

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Chemical Structure| 210353-53-0 同义名 : LB-20304a;SB-265805S;Gemifloxacin (mesylate);LB20304 mesylate;SB265805 mesylate
CAS号 : 210353-53-0
货号 : A538822
分子式 : C19H24FN5O7S
纯度 : 99%+
分子量 : 485.487
MDL号 : MFCD08277637
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(216.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(102.99 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Gemifloxacin mesylate (GFM) is a synthetic broad-spectrum antibacterial agent[1]. Gemifloxacin is a fluoroquinolone antibacterial agent which has an enhanced affinity for topoisomerase IV. It has potent activity against most gram-positive bacteria, particularly streptococcus pneumoniae. Gemifloxacin is over 30-fold more active than ciprofloxacin and 4- to 8-fold more active than moxifloxacin against this pathogen. Gemifloxacin has excellent activity against Haemophilus influenzae and Moraxella catarrhalis, and is unaffected by beta-lactamase production. Atypical respiratory pathogens (Legionella, Mycoplasma and Chlamydia spp.) are highly susceptible to gemifloxacin. Oral gemifloxacin 320 mg/day produced bacteriological responses of 94.7% in patients with acute exacerbations of chronic bronchitis and 95% of patients with uncomplicated urinary tract infections[3]. DTH (Delayed type hypersensitivity) assay has shown the significant immune suppressant potential of gemifloxacin at 25 mg/kg dose and 75mg/kg dose in mice[4]. Gemifloxacin is microbiologically the most active fluoroquinolone against Streptococcus pneumoniae--the leading pathogen of CAP (community-acquired pneumonia)[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03535558 - Recruiting December 31, 2018 United States, New Jersey ... 展开 >> Janssen Investigative Site Recruiting Titusville, New Jersey, United States, 08560 收起 <<
NCT03479736 - Completed - United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 <<
NCT01881438 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.06mL

0.41mL

0.21mL

10.30mL

2.06mL

1.03mL

20.60mL

4.12mL

2.06mL
参考文献

[1]Paim CS, Führ F, Martins MT, et al. Structural elucidation of gemifloxacin mesylate degradation product. Biomed Chromatogr. 2016;30(3):459‐465

[2]El-Koussi WM, Atia NN, et al. HPTLC method for direct determination of gemifloxacin mesylate in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Sep 15;967:98-101.

[3]Lowe MN, Lamb HM. Gemifloxacin. Drugs. 2000;59(5):1137‐1148

[4]Umair M, Javeed A, Ghafoor A, Ashraf M. Immunomodulatory activities of gemifloxacin in mice. Iran J Basic Med Sci. 2016;19(9):985‐992

[5]Lode HM, Schmidt-Ionas M, Stahlmann R. Gemifloxacin for community-acquired pneumonia. Expert Opin Investig Drugs. 2008;17(5):779‐786