|2,3,5-三氯-N-(3,5-二氯-2-羟基苯基)-6-羟基苯甲酰胺|CsnPharm

CAS No.: 2277-92-1

Oxyclozanide/氯羟柳胺 Catalog No. CSN21778

Synonyms: Oxiclozanidum;Zanil;Oxyclozanid

Oxyclozanide is a salicylanilide anthelmintic drug.

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技术信息

生物活性

描述Oxyclozanide (OXZ) is a salicylanilide anthelmintic drug that mainly acts by uncoupling oxidative phosphorylation in flukes. Goats treated with LVM (levamisole)-OXZ combination at the recommended dose for sheep may result in a reduced efficacy, because of under-dosing, which may increase the risk of drug resistance in parasites^[1]. Oxyclozanide in combination with colistin increased the activity of colistin against Col-S and Col-R A. baumannii, P. aeruginosa and K. pneumoniae. Time-kill curves showed synergistic activity between oxyclozanide and colistin against these bacterial isolates. Moreover, Col-R (colistin-resistant) A. baumannii, P. aeruginosa and K. pneumoniae in the presence of oxyclozanide presented greater permeability and disruption of their cell wall than Col-S (colistin against colistin-susceptible) strains, without modification of their outer membrane protein profile^[2]. The LD50 of oxyclozanide was ~3,707 mg/kg body weight, and the lowest observed adverse effect level of oxyclozanide was at a dose of 74 mg/kg in rats^[3]. Oxyclozanide demonstrated in-vitro antibacterial activity against meticillin-resistant S. pseudintermedius^[4].
参考文献

[1] Gokbulut C, Yalinkilinc HS, Aksit D, Veneziano V. Comparative pharmacokinetics of levamisole-oxyclozanide combination in sheep and goats following per os administration. Can J Vet Res. 2014 Oct;78(4):316-20
[2] Ayerbe-Algaba R, Gil-Marqués ML, Miró-Canturri A, Parra-Millán R, Pachón-Ibáñez ME, Jiménez-Mejías ME, Pachón J, Smani Y. The anthelmintic oxyclozanide restores the activity of colistin against colistin-resistant Gram-negative bacilli. Int J Antimicrob Agents. 2019 Oct;54(4):507-512
[3] Wang W, Dong Z, Zhang J, Zhou X, Wei X, Cheng F, Li B, Zhang J. Acute and Subacute Toxicity Assessment of Oxyclozanide in Wistar Rats. Front Vet Sci. 2019 Sep 6;6:294
[4] Levinson MR, Blondeau JM, Rosenkrantz WS, Plowgian CB. The in vitro antibacterial activity of the anthelmintic drug oxyclozanide against common small animal bacterial pathogens. Vet Dermatol. 2019 Aug;30(4):314-e87

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4909 mL
- 12.4546 mL
- 24.9093 mL
- 5 mM
- 0.4982 mL
- 2.4909 mL
- 4.9819 mL
- 10 mM
- 0.2491 mL
- 1.2455 mL
- 2.4909 mL

技术信息

CAS号

2277-92-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H6Cl5NO3

运输

蓝冰

分子量

401.46

别名

Oxiclozanidum;Zanil;Oxyclozanid;Zanilox;Diplin;ICI-46683;Oxiclozanida;氯羟柳胺

溶解度

DMSO	115.0 mg/mL (286.5 mM)
Water	insoluble

动物实验配方

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