Delafloxacin meglumine

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CAS NO:

352458-37-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

德拉沙星葡甲胺
ABT492 meglumine
RX-3341 meglumine
WQ-3034 meglumine

产品介绍

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) 是一种广谱氟喹诺酮类抗生素。Delafloxacin 具有广泛的活性，对耐药性的金黄色葡萄球菌，肺炎链球菌和肺炎克雷伯菌都有效。

生物活性

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinoloneantibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistantStaphylococcus aureus,Streptococcus pneumoniae, andKlebsiella pneumonia^[1].

IC₅₀& Target

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 againstS. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log₁₀CFU 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-log₁₀kill from initial burden for allS. aureusstrains^[1].
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)^[1].

Animal Model:	Mice with a neutropenic murine lung infection model (fourS. aureus, fourS. pneumoniae, and fourK. pneumoniaestrains)^[1]
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:	InhibitedS. aureusstrains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively. InhibitedS. pneumoniaestrains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively. InhibitedK. pneumoniastrains 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^[1]
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 mgoh/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.

Clinical Trial

分子量

635.97

性状

Solid

Formula

C₂₅H₂₉ClF₃N₅O₉

CAS 号

352458-37-8

中文名称

德拉沙星葡甲胺

运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据

In Vitro:

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。