产品说明书

Delafloxacin meglumine

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Chemical Structure| 352458-37-8 同义名 : RX-3341 meglumine;ABT492 meglumine;Delafloxacin (meglumine);Baxdela;WQ-3034;RX-3341;ABT-492;WQ-3034 meglumine
CAS号 : 352458-37-8
货号 : A587080
分子式 : C25H29ClF3N5O9
纯度 : 98%
分子量 : 635.974
MDL号 : MFCD26142921
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(7.86 mM)，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(78.62 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Delafloxacin meglumine is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia. Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log10 kill from initial burden for all S. aureus strains[2]. Delafloxacin meglumine is used for the treatment of acute bacterial skin and skin structure infections on the basis of data from two phase III trials. Delafloxacin is administered via both oral and parenteral routes. It has potent activity against methicillin-resistant Staphylococcus aureus and Streptococci, and is also effective against Enterobacteriaceae and Pseudomonas aeruginosa[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.86mL

1.57mL

0.79mL

15.72mL

3.14mL

1.57mL
参考文献

[1]Gunderson SM, Hayes RA, et al. In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis. Antimicrob Agents Chemother. 2004 Jan;48(1):203-8.

[2]Lepak AJ, Andes DR. In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model. Antimicrob Agents Chemother. 2016;60(8):4764‐4769.

[3]Kaul G, Kapoor E, Dasgupta A, Chopra S. Delafloxacin meglumine for the treatment of acute bacterial skin and skin structure infections (ABSSSI). Drugs Today (Barc). 2018;54(11):657‐666