352458-37-8|德拉沙星葡甲胺|Delafloxacin meglumine|MFCD26142921-范德生物科技公司

德拉沙星葡甲胺

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names：
Delafloxacin meglumine
CAS号：
352458-37-8
MDL Number： MFCD26142921
MF(分子式)： C25H29ClF3N5O9 MW(分子量)： 635.97
EINECS: Reaxys Number:
Pubchem ID:11578213 Brand:BIOFOUNT

德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)是第四代氟喹诺酮，对革兰氏阳性细菌以及非典型病原体具有增强的活性。Delafloxacin在治疗过程中与轻度ALT升高有关，但尚未与特发性急性肝损伤伴有症状和黄疸的情况相关联，正如其他氟喹诺酮类药物所描述的那样。

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YZM000170-10mg	10mg	99.98%	¥ 487.50	¥ 487.50		2-3天	- +	¥ 0.00

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中文别名	德拉沙星葡甲胺(352458-37-8);ABT492葡甲胺; RX-3341葡甲胺; WQ-3034葡甲胺;德拉沙星中间体1;来氟沙星葡甲胺;德拉福沙星葡甲胺;德拉沙星葡甲胺盐; 1-(6-氨基-3,5-二氟-2-吡啶基)-8-氯-6-氟-1,4-二氢-7-(3-羟基-1-氮杂环丁基)-4-氧代-3-喹啉羧酸葡甲胺盐;德拉沙星N-甲基葡萄糖胺盐;德拉沙星葡甲胺盐;地拉沙星葡甲胺;德拉沙星葡甲胺;巴克斯德拉 1-（6-氨基-3,5-二氟吡啶-2-基）-8-氯-6-氟-7-（3-羟基氮杂环丁烷-1-基）-4-氧喹啉-3-羧酸;（2R， 3R，4R，5S）-6-（甲基氨基）己烷-1,2,3,4,5-戊醇;
英文别名	Delafloxacin meglumine(352458-37-8);ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine;Baxdela; D-Glucitol,1-deoxy-1-(methylamino)-,1-(6-amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-3-quinolinecarboxylate (salt); 1-Deoxy-1-(methylamino)-D-glucitol 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate (salt); 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;ABT-492 MegluMine;100850;ABT492meglumine(Delafloxacinmeglumine);Delafloxacinmeglumine(ABT492meglumine;(2R,3R,4R,5S)-2,3,4,5-tetrahydroxy-6-(MethylaMino)hexyl1-(6-aMino-3,5-difluoropyridChemicalbookin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate;ABT492MegluMine;ABT492MegluMine;ABT-492MegluMine;Delafloxacin(MegluMine); Baxdela; 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；
CAS号	352458-37-8
SMILES	O=C(C1=CN(C2=NC(N)=C(F)C=C2F)C3=C(C=C(F)C(N4CC(O)C4)=C3Cl)C1=O)O.O[C@H]([C@H]([C@@H]([C@@H](CO)O)O)O)CNC
Inchi	InChI=1S/C18H12ClF3N4O4.C7H17NO5/c19-12-13-7(1-9(20)14(12)25-3-6(27)4-25)15(28)8(18(29)30)5-26(13)17-11(22)2-10(21)16(23)24-17;1-8-2-4(10)6(12)7(13)5(11)3-9/h1-2,5-6,27H,3-4H2,(H2,23,24)(H,29,30);4-13H,2-3H2,1H3/t;4-,5+,6+,7+/m.0/s1
InchiKey	AHJGUEMIZPMAMR-WZTVWXICSA-N
分子式 Formula	C25H29ClF3N5O9
分子量 Molecular Weight	635.97
闪点 FP
熔点 Melting point	No data available
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility	生物体外In Vitro:DMSO溶解度≥ 6.4 mg/mL(10.06 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性状	固体粉末,Power
储藏条件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)毒理性质：

Delafloxacin, like other fluoroquinolones, is associated with a low rate (3% to 4%) of serum enzyme elevations during therapy. These abnormalities are generally mild, asymptomatic and transient, resolving even with continuation of therapy. ALT elevations above 5 times the upper limit of normal occur in 1% or less of subjects. Although delafloxacin may not have been clearly linked to cases of clinically apparent liver injury, the other fluoroquinolones, such as ciprofloxacin, levofloxacin and moxifloxacin, rank among the 25 most common causes of drug induced liver injury in many case series. Estimates of the frequency of liver injury from fluoroquinolones have been 1:15,000 to 1:25,000 exposed persons. Delafloxacin has been in clinical use for a short time only, but is likely to have a similar frequency and pattern of liver injury as the other fluoroquinolones. The typical presentation of fluoroquinolone associated liver injury is with a short latency (1 day to 3 weeks) and abrupt onset with nausea, fatigue, abdominal pain and jaundice. The pattern of serum enzyme elevations can be either hepatocellular or cholestatic, cases with the shorter times to onset usually being more hepatocellular. In addition, the onset of illness may occur a few days after the medication is stopped. Many (but not all) cases have prominent allergic manifestations with fever and rash, and the liver injury may occur in the context of a generalized hypersensitivity reaction. Autoantibodies are usually not present. Most reported cases of liver injury from fluoroquinolones have been mild and self-limited, with recovery in 4 to 8 weeks from onset. However, the fatality rate of cases with jaundice has been greater than 10%. In addition, cases with a cholestatic pattern of serum enzymes may run a prolonged course and, in rare instances, have progressed to chronic vanishing bile duct syndrome leading to liver failure. Nevertheless, delafloxacin is a relatively recently introduced antibiotic and has yet to be convincingly linked to instances of acute hepatitis or jaundice. Likelihood score: E* (unproven but suspected cause of clinically apparent liver injury).

德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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产品说明	德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)是广谱的氟喹诺酮类抗生素
Introduction	Delafloxacin meglumine (ABT492 meglumine; RX341 meglumine; WQ034 meglumine) is a broadpectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drugesistantStaphylococcus aureus,Streptococcus pneumoniae, andKlebsiella pneumonia.
Application1	德拉沙星葡甲胺可用于细菌性皮肤和皮肤结构感染的治疗（ABSSSI）
Application2	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。
Application3

德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)药理学：

1、德拉沙星葡甲胺是氟喹诺酮类抗生素。IC50值：耐左氧氟沙星的肺炎链球菌菌株的MIC范围为0.0078至0.125 micro g / ml；目标：抗菌；ABT-492对喹诺酮敏感和耐药的革兰氏阳性生物更有效，对环丙沙星家族肠杆菌科某些成员的活性与环丙沙星相似，对喹诺酮敏感，非发酵性，革兰氏阴性生物的活性相当。体外：ABT-492对用MICs测试的所有326种需氧和厌氧窦穿刺窦分离物均表现出优异的体外活性（以微克/毫升计），其中90％的分离物被抑制如下：流感嗜血杆菌，0.001；卡他莫拉氏菌0.008; 和肺炎链球菌，0.015 。

2、德拉沙星葡甲胺是一种氟喹诺酮，可用于治疗成年患者的急性细菌性皮肤和皮肤结构感染（ABSSSI）。研究表明，德拉沙星葡甲胺对肝脏和肾脏具有优异的耐受性和低毒性。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

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. Antimicr

德拉沙星葡甲胺(352458-37-8,Delafloxacin,ABT492 meglumine,RX-3341 meglumine,WQ-3034 meglumine)参考文献：

1、Delafloxacin meglumine for the treatment of acute bacterial skin and skin structure infections (ABSSSI)
G Kaul 1, E Kapoor 1, A Dasgupta 1, S Chopra

Abstract Delafloxacin meglumine (Baxdela, WQ-3034, ABT-492, RX-3341; Melinta Therapeutics) was approved by the U.S. Food and Drug Administration (FDA) in June 2017 for the treatment of acute bacterial skin and skin structure infections on the basis of data from two phase III trials. Delafloxacin is a broad-spectrum anionic fluoroquinolone and its distinct chemical structure increases its potency in acidic environments. It is known to inhibit DNA replication and repair by targeting DNA gyrase and topoisomerase IV. 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. Delafloxacin is currently in phase III evaluation for treatment of community-acquired pneumonia and was classified as a qualified infectious disease product by the U.S. FDA in its approval.

2、In Vivo Pharmacodynamic Target Assessment of Delafloxacin against Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae in a Murine Lung Infection Model
Alexander J Lepak 1, David R Andes 2

Abstract Delafloxacin is a broad-spectrum anionic fluoroquinolone under development for the treatment of bacterial pneumonia. The goal of the study was to determine the pharmacokinetic/pharmacodynamic (PK/PD) targets in the murine lung infection model for Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumoniae Four isolates of each species were utilized for in vivo studies: for S. aureus, one methicillin-susceptible and three methicillin-resistant isolates; S. pneumoniae, two penicillin-susceptible and two penicillin-resistant isolates; K. pneumoniae, one wild-type and three extended-spectrum beta-lactamase-producing isolates. MICs were determined using CLSI methods. A neutropenic murine lung infection model was utilized for all treatment studies, and drug dosing was by the subcutaneous route. Single-dose plasma pharmacokinetics was determined in the mouse model after administration of 2.5, 10, 40, and 160 mg/kg. For in vivo studies, 4-fold-increasing doses of delafloxacin (range, 0.03 to 160 mg/kg) were administered every 6 h (q6h) to infected mice. Treatment outcome was measured by determining organism burden in the lung (CFU counts) at the end of each experiment (24 h). The Hill equation for maximum effect (Emax) was used to model the dose-response data. The magnitude of the PK/PD index, the area under the concentration-time curve over 24 h in the steady state divided by the MIC (AUC/MIC), associated with net stasis and 1-log kill endpoints was determined in the lung model for all isolates. MICs ranged from 0.004 to 1 mg/liter. Single-dose PK parameter ranges include the following: for maximum concentration of drug in serum (Cmax), 2 to 70.7 mg/liter; AUC from 0 h to infinity (AUC0-∞), 2.8 to 152 mg · h/liter; half-life (t1/2), 0.7 to 1 h. At the start of therapy mice had 6.3 ± 0.09 log10 CFU/lung. In control mice the organism burden increased 2.1 ± 0.44 log10 CFU/lung over the study period. There was a relatively steep dose-response relationship observed with escalating doses of delafloxacin. Maximal organism reductions ranged from 2 log10 to more than 4 log10 The median free-drug AUC/MIC magnitude associated with net stasis for each species group was 1.45, 0.56, and 40.3 for S. aureus, S. pneumoniae, and K. pneumoniae, respectively. AUC/MIC targets for the 1-log kill endpoint were 2- to 5-fold higher. Delafloxacin demonstrated in vitro and in vivo potency against a diverse group of pathogens, including those with phenotypic drug resistance to other classes. These results have potential relevance for clinical dose selection and evaluation of susceptibility breakpoints for delafloxacin for the treatment of lower respiratory tract infections involving these pathogens.

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