Nitroxoline
(Synonyms: 硝羟喹啉; 8-Hydroxy-5-nitroquinoline; 5-Nitro-8-quinolinol) 目录号 : GC11365An 8-hydroxyquinoline with diverse biological activities
Cas No.:4008-48-4
Sample solution is provided at 25 µL, 10mM.
Nitroxoline has been clinically used since 1962 for the treatment of urinary tract infections, especially those caused by gram negative bacilli. The current renewal of nitroxoline is due to its recently found activity against fungi, U. urealyticum, Mycoplasma, and Trichomonas.
In vitro: The machnistic study showed that nitroxoline, in the treatment of acute or recurrent urinary tract infections caused by Escherichia coli, could be decreased in the presence of Mg2+ and Mn2+ but not Ca2+. Moreover, with the divalent metal ions, a shift in the nitroxoline A448 indicated the formation of drug-ion complexes and a clear correlation was observed between the chelating property and antibacterial activity of nitroxolinet. In addition, it was found that the uptake was energy-independent and with biphasic kinetics: a rapid cell association phase and then a slower increase of cell- nitroxoline association [1].
In vivo: Previous animal study showed that nitroxoline suspension with Tween-80 in a could decrease the tone of the rat and guinea-pig ileum and diminish their peristalsis. Moreover, when administered orally in a dose 50 mg/kg to rats, nitroxoline was able to inhibit the agar-, serotonin-, as well as carrageenin-induced edemas of the rat paws without affecting the response to subplantar histamine injection [2].
Clinical trial: Twelve children were treated with nitroxoline (200 mg/kg/d) during 10 days for urinary tract infection. The results showed eight clinical and bacteriological success, one true failure, and three failure because of a non-compliance to the nitroxoline treatment. In addition, there was no qualitative and quantitative modification of the fecal flora observed after nitroxoline treatment [3].
References:
[1] Pelletier C,Prognon P,Bourlioux P. Roles of divalent cations and pH in mechanism of action of nitroxoline against Escherichia coli strains. Antimicrob Agents Chemother.1995 Mar;39(3):707-13.
[2] Zaks AS,Zil'ber AL,Kapitonenko TA. Spasmolytic and anti-inflammatory activity of 8-hydroxyquinolines. Farmakol Toksikol.1984 Sep-Oct;47(5):44-7.
[3] Lambert-Zechovsky N,Lévêque B,Bingen E,Pillion G,Chapelle J,Mathieu H. Clinical study and effect of nitroxoline on fecal flora in childrenPathol Biol (Paris).1987 May;35(5):669-72.
Cas No. | 4008-48-4 | SDF | |
别名 | 硝羟喹啉; 8-Hydroxy-5-nitroquinoline; 5-Nitro-8-quinolinol | ||
化学名 | 5-nitroquinolin-8-ol | ||
Canonical SMILES | OC1=C2C(C=CC=N2)=C(N(=O)=O)C=C1 | ||
分子式 | C9H6N2O3 | 分子量 | 190.16 |
溶解度 | DMF: 25 mg/ml,DMSO: 30 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 0.5 mg/ml | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 5.2587 mL | 26.2936 mL | 52.5873 mL |
5 mM | 1.0517 mL | 5.2587 mL | 10.5175 mL |
10 mM | 0.5259 mL | 2.6294 mL | 5.2587 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.50%
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