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Temafloxacin (hydrochloride)

 
Catalog No.
C5429
氟喹诺酮类抗生素
组合的产品项目
规格价格库存 数量
5mg
¥ 2,275.00
Ship with 10-15 days
10mg
¥ 3,304.00
Ship with 10-15 days
25mg
¥ 4,766.00
Ship with 10-15 days

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A

背景

MIC90: less than or equal to 0.06 micrograms/mL respiratory pathogens

Temafloxacin is a fluoroquinolone antibiotic.

Fluoroquinolone antibiotic is an organonitrogen heterocyclic antibiotic with a quinolone or quinolone-like moiety and have a fluorine atom attached to the central ring system.

In vitro: The in-vitro activities of temafloxacin, ciprofloxacin, and ofloxacin against gram-negative bacteria were compared. The 90% minimal inhibitory concentrations (MIC90s) of temafloxacin for respiratory pathogens were less than or equal to 0.06 micrograms/mL. Temafloxacin was also active against bacterial agents of sexually transmitted diseases, such as Neisseria gonorrhoeae and Chlamydia trachomatis [1].

In vivo: Mixed aerobic-anaerobic infection was induced by i.p. implantation of gelatin capsules containing Bacteroides fragilis, Escherichia coli, and sterile rat faeces. Temafloxacin was found to be highly active with a 90.9% cure rate in comparison with no treatment, and as active as a combination of clindamycin and gentamicin. Temafloxacin at 12 mg/dose resulted in rise to serum concentrations exceeding the MIC values of both microorganisms for at least 8 h [2].

Clinical trial: Clinical studies showed that temafloxacin has improved activity against pneumococci. Eradication rates in acute exacerbations of chronic bronchitis collated from individual studies are 98% overall and 100% in pneumococcal infections. Moreover, eradication rates in smokers and the elderly illustrate significant advantages for temafloxacin. In pneumonia, a twice-daily temafloxacin regimen has given equivalent overall results to those of amoxycillin (84.6% vs 80%) [3].

References:
[1] Hardy DJ.  In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S.
[2] Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S.  Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92.
[3] Ball P. The role of temafloxacin in the community setting: an overview. J Antimicrob Chemother. 1991 Dec;28 Suppl C:121-30.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt453.8
Cas No.105784-61-0
FormulaC21H18F3N3O3·HCl
SynonymsA-62254
Solubility≤2mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, monohydrochloride
SDFDownload SDF
Canonical SMILESCC1CN(C2=C(F)C=C(C(C(C(O)=O)=CN3C4=CC=C(F)C=C4F)=O)C3=C2)CCN1.Cl
运输条件 蓝冰运输或根据您的需求运输。
一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

细胞实验 [1]:

细胞系

流感嗜血杆菌,卡他莫拉氏菌,百日咳博德特氏菌, 副百日咳博德特氏菌,脑膜炎奈瑟菌

溶解方法

在DMSO中的溶解度≤2mg/ml。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

0~2 μg/ml

应用

Temafloxacin对呼吸道病原体如流感嗜血杆菌,卡他莫拉菌,脑膜炎奈瑟菌,百日咳博德特氏菌和嗜肺军团菌的最低抑菌浓度为(MIC90s)≤0.06 μg/ mL。Temafloxacin还具有抵抗性传播疾病细菌的作用,包括淋病奈瑟菌(MIC90≤0.015μg/ mL)和沙眼衣原体(MIC90 0.25μg/ mL)。

动物实验 [2]:

动物模型

大鼠腹腔内脓肿模型

剂量

12 mg/dose

应用

与未经治疗相比,发现temafloxacin具有很高的活性,治愈率为90.9%,并且与克林霉素和庆大霉素的组合活性相当。剂量为12 mg /剂的temafloxacin导致血清浓度升高,超过至少8h的两种微生物的MIC值。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Hardy DJ. In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S. doi: 10.1016/0002-9343(91)90304-g. PMID: 1662890.

[2]. Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S. Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92. doi: 10.1093/jac/29.6.687. PMID: 1324241.

质量控制

质量控制和MSDS

批次:

化学结构

Temafloxacin (hydrochloride)