Oxyclozanide

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Chemical Structure| 2277-92-1 同义名 : 氧氯氮酰胺 ;Zanil; Oxiclozanidum; Oxiclozanida; ICI 46683; Diplin; Zanilox; Oxyclozanid
CAS号 : 2277-92-1
货号 : A250572
分子式 : C13H6Cl5NO3
纯度 : 98%
分子量 : 401.46
MDL号 : MFCD00864507
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: 105 mg/mL(261.55 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
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.45mL

2.49mL

1.25mL

24.91mL

4.98mL

2.49mL
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