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Delafloxacin

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Chemical Structure| 189279-58-1 同义名 : ABT492;RX-3341;RX-3341J;WQ-3034
CAS号 : 189279-58-1
货号 : A139239
分子式 : C18H12ClF3N4O4
纯度 : 98%
分子量 : 440.76
MDL号 : MFCD09955301
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(238.22 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
动物实验配方：
生物活性
描述 Pneumonia is one of the most common infectious diseases encountered worldwide. The major pathogen of community-acquired pneumonia (CAP) continues to be S. pneumoniae. In the hospital setting, S. aureus and Gram-negative bacteria are more commonly encountered and are frequently drug resistant. Delafloxacin is a novel fluoroquinolone antibiotic in development for the treatment of respiratory tract infections. It has a broad spectrum of activity that includes drug-resistant S. aureus, S. pneumoniae, and Klebsiella pneumoniae. The lowest MICs were observed for S. aureus (range, 0.004 to 0.008 mg/liter). The in vitro potency against S. pneumoniae and K. pneumoniae strains was more varied (range, 0.016 to 0.125 mg/liter and 0.06 to 1 mg/liter, respectively). As for pharmacokinetics, exposure to delafloxacin increased in a dose-dependent manner across the dose range. Cmax concentrations ranged from 2 to 71 mg/liter. AUC0–∞ values ranged from 2.8 to 152 mg · h/liter and were linear across the 2.5- to 160-mg dosing range (R2 of 0.99). The elimination half-life ranged from 0.7 to 1 h[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.34mL

2.27mL

1.13mL

22.69mL

4.54mL

2.27mL
参考文献

[1]Gunderson SM, Hayes RA, Quinn JP, 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]Goldstein EJ, Citron DM, et al. In vitro activities of ABT-492, a new fluoroquinolone, against 155 aerobic and 171 anaerobic pathogens isolated from antral sinus puncture specimens from patients with sinusitis. Antimicrob Agents Chemother. 2003 Sep;47(9):3008-11.

[3]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