Temafloxacin(hydrochloride)

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

105784-61-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	453.8
Cas No.	105784-61-0
Formula	C₂₁H₁₈F₃N₃O₃·HCl
Synonyms	A-62254
Solubility	≤2mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name	1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, monohydrochloride
Canonical SMILES	CC1CN(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	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。

资料参考

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.

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.