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Nalidixic acid sodium salt

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Chemical Structure| 3374-05-8 同义名 : 萘啶酸 钠盐
CAS号 : 3374-05-8
货号 : A783659
分子式 : C12H11N2NaO3
纯度 : 98%
分子量 : 254.217
MDL号 : MFCD00064376
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 120 mg/mL(472.04 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Nalidixic acid sodium salt, a quinolone antibiotic, is effective against both gram-positive and gram-negative bacteria. Nalidixic acid acts in a bacteriostatic manner in lower concentrations and is bactericidal in higher concentrations. Nalidixic acid inhibits a subunit of DNA gyrase and topoisomerase IV and reversibly blocks DNA replication in susceptible bacteria. Nalidixic acid is against with Escherichia coli, Pasteurella spp., Klebsiella pneuiiioniae, Aerobacter aeroyenes, Proteus spp., Salmonella spp., Shigella spp. and Brucella spp. with MIC values of 5.0-12.5 μg/ml, 0.5-2.5 μg/ml, 0.8-25.0 μg/ml, 1.0-25.0 μg/ml, 1.25-30.0 μg/ml, 8-3.2 μg/ml, and 7.5-10.0 μg/ml, respectively. Maximal activity is observed against systemic infections caused by E. coli, A. aerobacter, Proteus mirabilis, Shigella fkxneri, the ED50 values are 25 mg/kg, 60 mg/kg, 50 mg/kg, and 62 mg/kg, respectively. The acute toxicity (LD50) of Nalidixic acid in mice following oral and parenteral administration is: oral, 3300 mg/kg; intravenous, 176 mg/kg; and subcutaneous, 500 mg/kg[3]. The MIC of nalidixic acid was 700 μg/mL against P. aeruginosa. The present findings suggest that the morphology and protein expression of P. aeruginosa is greatly affected by nalidixic acid[4]. Nalidixic acid is metabolized by hydroxylation to 7-hydroxymethylnalidixic acid and then by oxidation to 7-carboxynalidixic acid. The half-lives of the two elimination phases of nalidixic acid are 0.75 and 2.5 h[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.67mL

3.93mL

1.97mL

39.34mL

7.87mL

3.93mL

参考文献

[1]G Y LESHER,et al. 1,8-NAPHTHYRIDINE DERIVATIVES. A NEW CLASS OF CHEMOTHERAPEUTIC AGENTS. J Med Pharm Chem. 1962 Sep;91:1063-5.

[2]Anna Fàbrega, et al. Mechanism of Action of and Resistance to Quinolones. Microb Biotechnol

[3]Fàbrega A, Madurga S, Giralt E, Vila J. Mechanism of action of and resistance to quinolones. Microb Biotechnol. 2009 Jan;2(1):40-61

[4]Al Bahry S, Sivakumar N, Al-Khambashi M. Effect of nalidixic acid on the morphology and protein expression of Pseudomonas aeruginosa. Asian Pac J Trop Med. 2012 Apr;5(4):265-9

[5]Vree TB, Wijnands WJ, Baars AM, Hekster YA. Pharmacokinetics of nalidixic acid in man: hydroxylation and glucuronidation. Pharm Weekbl Sci. 1988 Oct 14;10(5):193-9