Delafloxacin meglumine|352458-37-8|(德拉沙星葡甲胺; ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine)-陌孚医药/Medlife

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Delafloxacin meglumine (Synonyms: 德拉沙星葡甲胺; ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine)

目录号: PC12829 纯度: ≥98%

CAS No. :352458-37-8

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中文名称	Delafloxacin meglumine
中文别名	德拉沙星N-甲基葡萄糖胺盐;德拉沙星中间体1
英文名称	Delafloxacin meglumine
英文别名	ABT-492 Meglumine;(2R,3R,4R,5S)-2,3,4,5-Tetrahydroxy-6-(methylamino)hexyl 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquin;1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-c;1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid,(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol;Delafloxacin meglumine
Cas No.	352458-37-8
分子式	C₁₈H₁₂N₄O₄F₃Cl^.C₇H₁₇NO₅
分子量	635.97
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 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.

性状

Solid

IC50 & Target[1][2]

Quinolone

体内研究(In Vivo)

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.
Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t_1/2=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively).

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

Animal Model:	Mice with a neutropenic murine lung infection model (four S. aureus, four S. pneumoniae, and four K. pneumoniae strains)
Dosage:	The total daily doses vary from 0.156 to 640 mg/kg/24 h
Administration:	0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection
Result:	Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively. Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively. Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively.

Animal Model:	Neutropenic mice
Dosage:	2.5, 10, 40, and 160 mg/kg; 0.2 mL
Administration:	Subcutaneous injection; 24 h
Result:	The maximum drug concentrations (C_max) concentrations ranged from 2 to 71 mg/L. AUC_0-∞ values ranged from 2.8 to 152 mg?h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t_1/2) ranged from 0.7 to 1 h.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

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

ClinicalTrial

参考文献

[1]. Lepak AJ, et al. 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 Jul 22;60(8):4764-9. [Information]

溶解度数据

体外研究:

H₂O : 50 mg/mL (78.62 mM; Need ultrasonic)

DMSO : ≥ 6.4 mg/mL (10.06 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5724 mL	7.8620 mL	15.7240 mL
5 mM	0.3145 mL	1.5724 mL	3.1448 mL
10 mM	0.1572 mL	0.7862 mL	1.5724 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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