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抑制剂描述:

产品名称:Levofloxacin

产品别名:见爱必信官网

英文别名:Levofloxacin

靶点:Topoisomerase

CAS:100986-85-4

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Levofloxacin (Levaquin) is a synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. Levofloxacin inhibits bacterial type II topoisomerases, topoisomerase IV and DNA gyrase. Levofloxacin, like other fluoroquinolones, inhibits the A subunits of DNA gyrase, two subunits encoded by the gyrA gene. This results in strand breakage on a bacterial chromosome, supercoiling, and resealing; DNA replication and transcription is inhibited.

溶解性:Ethanol :9 mg/mL (24.9 mM)
DMSO :23 mg/mL (63.6 mM)
Water :9 mg/mL (24.9 mM)

体外研究:

Levofloxacin is active against most aerobic Gram-positive and Gram-negative organisms and demonstrates moderate?activity?against anaerobes. Levofloxacin is two-fold more active than ciprofloxacin against Streptococcus pneumoniae and 2- to 4-fold more active than ciprofloxacin against Staphylococcus aureus, Xanthomonas maltophilia, and Bacteroides fragilis. Levofloxacin is two- to eightfold more?active?than ciprofloxacin against coagulase-negative staphylococci and Acinetobacter spp., although these improvements in potency may not be clinically relevant.?Levofloxacin?inhibits 90% of streptococci when it is used at concentrations of 1 mg/mL to 2 mg/mL. Levofloxacin?exhibits twofold greater?inhibitory?and?bactericidal?activities?than ofloxacin?against?either extracellular or intracellular tubercle bacilli.? Levofloxacin?has the least?inhibitory?effect on osteoblastic cell growth, with a 50%?inhibitory concentration of approximately 80 mg/mL at 48 and 72 hours. Levofloxacin results in strong inhibition of calcium deposition, as determined on day 14 by alizarin red staining and biochemical analysis. Levofloxacin inhibits glycosaminoglycan synthesis initially and DNA synthesis and mitochondrial function secondarily at actual arthropathic concentrations in cultured rabbit chondrocytes but that these changes are reversible and not enough to kill the cells.

体内研究:Levofloxacin is as efficacious as or more efficacious than that with ciprofloxacin in systemic as well as pyelonephritis infections in mice. Levofloxacin achieves higher concentrations in the serum and tissue of mice than does ciprofloxacin.

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