Oxolinic acid

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Chemical Structure| 14698-29-4 同义名 : 恶喹酸 ;NSC 110364;Urinox;Dioxacin;Prodoxol;Nidantin;Emyrenil
CAS号 : 14698-29-4
货号 : A203320
分子式 : C13H11NO5
纯度 : 98+%
分子量 : 261.23
MDL号 : MFCD00056775
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 1 mg/mL(3.83 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

动物实验配方:
生物活性
靶点
  • DNA synthesis

描述 Oxolinic Acid is an antibiotic against both Gram-negative and Gram-positive bacteria. Oxolinic acid can be used for the research of acute and chronic urinary tract infections. Oxolinic acid (2-5 ug/mL) inhibits 115 strains of E. coli. Oxolinic acid (0-31 ug/mL) inhibits 94 % of the 44 strains of Proteus mirabilis. Oxolinic acid (>5 ug/mL) inhibits all strains of Strept. Faecalis[3]. Oxolinic acid reduced RNA synthesis rates whether chromosome supercoiling decreased, increased, or remained unchanged[4]. Oxolinic acid induced benign Leydig cell tumours of the testis in rats at the highest dose level tested (1000 ppm). The no-effect level for tumour induction was confirmed to be 300 ppm (10.9 mg/kg/day) in rats. None was induced in mice[5]. The in vitro minimum inhibitory concentration (MIC) values of oxolinic acid against three strains of Vibrio anguillarum isolated from diseased cod were 0.016 microg mL(-1) (HI-610), 0.250 microg mL(-1) (HI-618) and 0.250 microg mL(-1) (HI-A21)[6]. Oxolinic acid induces Leydig cell tumors in rats by chronically stimulating the release of LH (luteinizing hormone) from the pituitary[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.83mL

0.77mL

0.38mL

19.14mL

3.83mL

1.91mL

38.28mL

7.66mL

3.83mL

参考文献

[1]Tarushi A, Psomas G, et al. Zinc complexes of the antibacterial drug oxolinic acid: structure and DNA-binding properties. J Inorg Biochem. 2009 Jun;103(6):898-905.

[2]Garcia de Mateos-Verchere J, Vaugeois JM, et al. Behavioural and neurochemical evidence that the antimicrobial agent oxolinic acid is a dopamine uptake inhibitor. Eur Neuropsychopharmacol. 1998 Dec;8(4):255-9.

[3]Kershaw MJ, Leigh DA. The antibacterial and pharmacological activity of oxolinic acid (Prodoxol). J Antimicrob Chemother. 1975 Sep;1(3):311-5

[4]Manes SH, Pruss GJ, Drlica K. Inhibition of RNA synthesis by oxolinic acid is unrelated to average DNA supercoiling. J Bacteriol. 1983 Jul;155(1):420-3

[5]Yamada T, Maita K, Nakamura J, Murakami M, Okuno Y, Hosokawa S, Matsuo M, Yamada H. Carcinogenicity studies of oxolinic acid in rats and mice. Food Chem Toxicol. 1994 May;32(5):397-408

[6]Samuelsen OB, Bergh O, Ervik A. A single-dose pharmacokinetic study of oxolinic acid and vetoquinol, an oxolinic acid ester, in cod, Gadus morhua L., held in sea water at 8 degrees C and in vitro antibacterial activity of oxolinic acid against Vibrio anguillarum strains isolated from diseased cod. J Fish Dis. 2003 Jun;26(6):339-47. doi: 10.1046/j.1365-2761.2003.00466.x. PMID: 12899409

[7]Yamada T, Nakamura J, Murakami M, Okuno Y, Hosokawa S, Matsuo M, Yamada H. The correlation of serum luteinizing hormone levels with the induction of Leydig cell tumors in rats by oxolinic acid. Toxicol Appl Pharmacol. 1994 Nov;129(1):146-54