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Nalidixic acid

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Chemical Structure| 389-08-2 同义名 : 萘啶酸 ;NSC 82174;WIN 18,320;Nalidixic Acid, Nevigramon, Neggram, Wintomylon, WIN 18,320
CAS号 : 389-08-2
货号 : A821895
分子式 : C12H12N2O3
纯度 : 98%
分子量 : 232.235
MDL号 : MFCD00006884
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(21.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(21.53 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • Topo II
描述 Nalidixic acid, synthetic 1,8-naphthyridine, is a spectrum antimicrobial agent. Nalidixic acid is against a variety of microorganisms, it 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. The in vivo activity of Nalidixic acid is most pronounced against Gram-negative bacteria, while Gram-positive organisms are generally more resistant. 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[2]. The MIC of nalidixic acid was 700 μg/mL against P. aeruginosa. The exposure of P. aeruginosa to different concentrations of nalidixic acid resulted in deformation of most of the growing cells. At the concentration of 600 μg/mL most of the cells turned into elongated and adhere to each other while some of the cells were bulged. The intensity of protein bands were changed when they exposed to nalidixic acid[3]. The combinations of nalidixic acid + methyl gallate/carvacrol improved nalidixic acid resistant pathogenic bacteria inhibition with synergy or partial synergy activity[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
NCT03190421 Urinary Tract Infections Not Applicable Recruiting December 30, 2019 United States, Illinois ... 展开 >> Loyola University Medical Center Recruiting Maywood, Illinois, United States, 60153 Contact: Mary J Tulke, RN    708-216-2067    mtulke@luc.edu 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.31mL

0.86mL

0.43mL

21.53mL

4.31mL

2.15mL

43.06mL

8.61mL

4.31mL
参考文献

[1]Emmerson AM, Jones AM. The quinolones: decades of development and use. J Antimicrob Chemother. 2003 May;51 Suppl 1:13-20.

[2]Crumplin GC, Smith JT. Nalidixic acid: an antibacterial paradox. Antimicrob Agents Chemother. 1975 Sep;8(3):251-61

[3]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

[4]Choi JG, Kang OH, Lee YS, Oh YC, Chae HS, Jang HJ, Shin DW, Kwon DY. Antibacterial activity of methyl gallate isolated from Galla Rhois or carvacrol combined with nalidixic acid against nalidixic acid resistant bacteria. Molecules. 2009 May 11;14(5):1773-80