Oxyclozanide
(Synonyms: 氯羟柳胺) 目录号 : GC32198
Oxyclozanide (Oxiclozanidum, Zanil, Oxyclozanid, Zanilox) is a salicylanilide anthelmintic and mitochondrial uncoupling anthelmintic drug approved for veterinary use.
Cas No.:2277-92-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oxyclozanide (Oxiclozanidum, Zanil, Oxyclozanid, Zanilox) is a salicylanilide anthelmintic and mitochondrial uncoupling anthelmintic drug approved for veterinary use.
| Cas No. | 2277-92-1 | SDF | |
| 别名 | 氯羟柳胺 | ||
| Canonical SMILES | O=C(NC1=CC(Cl)=CC(Cl)=C1O)C2=C(O)C(Cl)=CC(Cl)=C2Cl | ||
| 分子式 | C13H6Cl5NO3 | 分子量 | 401.46 |
| 溶解度 | DMSO : ≥ 100 mg/mL (249.09 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4909 mL | 12.4545 mL | 24.9091 mL |
| 5 mM | 0.4982 mL | 2.4909 mL | 4.9818 mL |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4909 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Acute and Subacute Toxicity Assessment of Oxyclozanide in Wistar Rats
Front Vet Sci 2019 Sep 6;6:294.PMID:31552282DOI:10.3389/fvets.2019.00294.
Oxyclozanide is an effective anthelmintic and has shown good properties in other ways including anti-adenovirus, anti-biofilm, antifungal, and antibacterial activity. This study aimed to investigate the acute and subacute 28-days repeated dose oral toxicity of an Oxyclozanide suspension in Wistar rats. A high oral lethal dose (LD50) of 3,707 mg/kg was observed in the acute toxicity test. During the 28-days time period, no obvious adverse effects or death were detected. Histopathological changes were observed in the heart, liver, and kidney of animals treated with high dose of Oxyclozanide. Based on the hematological parameters, there were no statistical differences between the oxyclozanide-treated group and the control group. For biochemistry assays, ALP, AST, GLU, TBIL, GLO, TG, BUN, UA, LDH, and CK were statistically changed in the treatment groups. These data suggested that the LD50 of Oxyclozanide was ~3,707 mg/kg body weight (BW), and the lowest observed adverse effect level (LOAEL) of Oxyclozanide was at a dose of 74 mg/kg in rats.
The anthelmintic Oxyclozanide restores the activity of colistin against colistin-resistant Gram-negative bacilli
Int J Antimicrob Agents 2019 Oct;54(4):507-512.PMID:31299296DOI:10.1016/j.ijantimicag.2019.07.006.
Due to the significant increase in antimicrobial resistance in Gram-negative bacilli (GNB), development of non-antimicrobial therapeutic alternatives, which can be used together with the few and non-optimal available antimicrobial agents such as colistin, has become an urgent need. In this context, dysregulation of the bacterial cell wall could be a therapeutic adjuvant to the activity of colistin. The aim of this study was to analyse the activity of Oxyclozanide, an anthelmintic drug, in combination with colistin against colistin-susceptible (Col-S) and colistin-resistant (Col-R) GNB. Three Col-S reference strains and 13 clinical isolates (1 Col-S, 12 Col-R) of Acinetobacter baumannii, Pseudomonas aeruginosa and Klebsiella pneumoniae were studied. Microdilution assays and time-kill curves were performed to examine the activity of Oxyclozanide in combination with colistin. The outer membrane protein (OMP) profile, membrane permeability and cell wall structure of Col-S and Col-R A. baumannii, P. aeruginosa and K. pneumoniae in the presence of Oxyclozanide were assessed by SDS-PAGE, fluorescence microscopy and transmission electron microscopy, respectively. 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 A. baumannii, P. aeruginosa and K. pneumoniae in the presence of Oxyclozanide presented greater permeability and disruption of their cell wall than Col-S strains, without modification of their OMP profile. These data suggest that combination of Oxyclozanide and colistin may be a new alternative for the treatment of Col-R GNB infections.
Determination and pharmacokinetics study of Oxyclozanide suspension in cattle by LC-MS/MS
BMC Vet Res 2019 Jun 24;15(1):210.PMID:31234851DOI:10.1186/s12917-019-1963-0.
Background: Oxyclozanide is an anthelmintic drug that is widely used to treat fasciolosis. However, the pharmacokinetics of Oxyclozanide in cattle are not yet clearly understood. The present study was designed to develop a sensitive method to determine Oxyclozanide levels in cattle plasma using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) and to study its pharmacokinetics for application in cattle. Results: A simple and rapid HPLC-MS/MS analytical method was established and validated to quantify Oxyclozanide levels in cattle plasma using niclosamide as the internal standard (IS) in negative ion mode. Chromatographic separation of the analytes was achieved using a C18 analytical column (75 脳 4.6 mm, 2.7 渭m) at 30 掳C. The mobile phase comprised 0.01% v/v acetic acid (HOAc) diluted in water:acetonitrile (MeCN) (90:10% v/v) and 5 mM ammonium formate in methanol (MeOH):MeCN (75:25, v/v) at a 10:90 ratio (v/v) and was delivered at a flow rate of 0.4 mL min- 1. A good linear response across the concentration range of 0.02048-25.600 渭g/mL was achieved (r2 = 0.994). The method was validated with respect to linearity, matrix effect, accuracy, precision, recovery and stability. The lower limit of quantification (LLOQ) was 0.020 渭g/mL, and the extraction recovery was > 98% for Oxyclozanide. The inter- and intra-day accuracy and precision of the method showed the relative standard deviation (RSD) less than 10%. The method was successfully applied to an assessment of the pharmacokinetics of Oxyclozanide in cattle plasma. In healthy cattle, a single oral dose of an Oxyclozanide suspension followed the one-compartment model, with a half-life (T1/2) of 64.40 卤 30.18 h, a plasma clearance rate (CL/F) of 11.426 卤 2.442 mL/h/kg, and an average area under the curve (AUC) of 965.608 卤 220.097 h*渭g/mL. The peak concentration (Cmax) was 15.870 卤 2.855 渭g/mL, which occurred at a peak time (Tmax) = 22.032 卤 3.343 h. Conclusions: A reliable, accurate HPLC-MS/MS analytical method was established in our study and successful applied to study the pharmacokinetics of Oxyclozanide in cattle plasma. These results will be useful for further evaluations of the pharmacokinetic properties of Oxyclozanide or for monitoring therapeutic drugs in animals.
Efficacy of Oxyclozanide and Closantel against Rumen Flukes (Paramphistomidae) in Naturally Infected Sheep
Animals (Basel) 2020 Oct 22;10(11):1943.PMID:33105640DOI:10.3390/ani10111943.
Paramphistomosis is considered an emergent disease of ruminants in Europe. Some drugs have been found effective for treating paramphistomid infections in cattle, but data in sheep are currently limited. Thus, faecal samples from 25 adult sheep naturally infected with paramphistomids were collected weekly to test the efficacy of Oxyclozanide and closantel. Three groups were performed: nine animals orally treated with a single dose of Oxyclozanide (15 mg/kg bodyweight (BW) integrated the G-OXI group, whereas eight sheep orally treated with a single dose of closantel (10 mg/kg BW) were placed in a group called G-CLS. Eight untreated controls constituted the group G-CON. Oxyclozanide showed efficacies up to 90% until week 11 post-treatment, with a maximum efficacy of 98.3%, and significant differences were found between G-OXI and G-CON until the 26th week post-treatment. Closantel was insufficiently active (0-81%) throughout the study and differences compared to G-CON were never found. The present study reveals that Oxyclozanide given at a single oral dose of 15 mg/kg BW is highly effective against adult rumen flukes in sheep. In addition, the use of a single oral dose of closantel at 10 mg/kg BW is not recommended for treating paramphistomid infections in sheep.
The ionophore Oxyclozanide enhances tobramycin killing of Pseudomonas aeruginosa biofilms by permeabilizing cells and depolarizing the membrane potential
J Antimicrob Chemother 2019 Apr 1;74(4):894-906.PMID:30624737DOI:10.1093/jac/dky545.
Objectives: To assess the ability of Oxyclozanide to enhance tobramycin killing of Pseudomonas aeruginosa biofilms and elucidate its mechanism of action. Methods: Twenty-four hour biofilms formed by the P. aeruginosa strain PAO1 and cystic fibrosis (CF) isolates were tested for susceptibility to Oxyclozanide and tobramycin killing using BacTiter-Glo鈩?and cfu. Biofilm dispersal was measured using crystal violet staining. Membrane potential and permeabilization were quantified using DiOC2(3) and TO-PRO-3, respectively. Results: Here we show that the ionophore anthelmintic Oxyclozanide, combined with tobramycin, significantly increased killing of P. aeruginosa biofilms over each treatment alone. This combination also significantly accelerated the killing of cells within biofilms and stationary phase cultures and it was effective against 4/6 CF clinical isolates tested, including a tobramycin-resistant strain. Oxyclozanide enhanced the ability of additional aminoglycosides and tetracycline to kill P. aeruginosa biofilms. Finally, Oxyclozanide permeabilized cells within the biofilm, reduced the membrane potential and increased tobramycin accumulation within cells of mature P. aeruginosa biofilms. Conclusions: Oxyclozanide enhances aminoglycoside and tetracycline activity against P. aeruginosa biofilms by reducing membrane potential, permeabilizing cells and enhancing tobramycin accumulation within biofilms. We propose that Oxyclozanide counteracts the adaptive resistance response of P. aeruginosa to aminoglycosides, increasing both their maximum activity and rate of killing. As Oxyclozanide is widely used in veterinary medicine for the treatment of parasitic worm infections, this combination could offer a new approach for the treatment of biofilm-based P. aeruginosa infections, repurposing Oxyclozanide as an anti-biofilm agent.