Fluazuron
(Synonyms: 吡虫隆) 目录号 : GC43678
An acaricide
Cas No.:86811-58-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fluazuron is an acaricide widely-used to control tick populations in cattle, sheep, and pigs. Fluazuron inhibits chitin formation limiting viable egg production and prevents immature ticks from moulting. It is effective against populations of R. microplus, R. sanguineus, S. scabei, and Y. pestis at host doses ranging from 1.5 to 100 mg/kg. Fluazuron does not effect populations of F. candida or O. gazella, alleviating concerns about non-specific insecticide activity. Resistance to fluazuron in certain R. microplus strains may be emerging.
| Cas No. | 86811-58-7 | SDF | |
| 别名 | 吡虫隆 | ||
| Canonical SMILES | FC1=C(C(NC(NC2=CC(OC3=C(Cl)C=C(C(F)(F)F)C=N3)=C(Cl)C=C2)=O)=O)C(F)=CC=C1 | ||
| 分子式 | C20H10Cl2F5N3O3 | 分子量 | 506.2 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | 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 | 1.9755 mL | 9.8775 mL | 19.755 mL |
| 5 mM | 0.3951 mL | 1.9755 mL | 3.951 mL |
| 10 mM | 0.1976 mL | 0.9878 mL | 1.9755 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。
The efficacy of Fluazuron in the management of blowfly strike in sheep
Exp Parasitol 2022 May-Jun;236-237:108251.PMID:35398341DOI:10.1016/j.exppara.2022.108251.
The blowflies Lucilia spp. and Chryomya spp. feature prominently as a leading cause of myiasis and production losses in sheep in South Africa. With chemical means of preventing and treating blowfly strike being a common manner of control, new molecules or formulations effective against blowfly strike are needed as resistance becomes more of a problem. For this study we evaluated the potential of topical application of Fluazuron on sheep as an additional means to control blowflies. When pure Fluazuron was applied to raw meat at the recommended dose for cattle, significant effects on adult fly development were observed. However when applied topically to post-mortally collected sheep pelts at the same dose rate, no significant effects were observed on larval repellence or larval development with fly development progressing as expected. A subsequent pharmacokinetic study showed virtually no systemic absorption together with significant wool binding. Despite demonstrating that Fluazuron was effective against blowfly larvae, wool binding of the molecule preclude its use.
Fluazuron orally administered to guinea pigs: pharmacokinetic and efficacy against Amblyomma sculptum
Parasit Vectors 2022 Jun 10;15(1):198.PMID:35689268DOI:10.1186/s13071-022-05325-4.
Background: Brazilian spotted fever (BSF), the most lethal tick-borne disease in the Western Hemisphere, is caused by the bacterium Rickettsia rickettsii and transmitted by the bite of Amblyomma sculptum. Capybaras are considered primary hosts of this tick and amplifier hosts of R. rickettsii, generating new infected lineages of A. sculptum in BSF-endemic areas. To define a possible treatment regimen for controlling the tick A. sculptum in capybaras, the aim of this study was to establish an effective Fluazuron (FLU) dose to control A. sculptum larvae in artificially infested guinea pigs. Methods: In Study I (pharmacokinetic and pharmacodynamic analysis), 24 guinea pigs were divided into four equal groups: control group (CG; untreated) and treated groups receiving FLU administered by gavage in three doses: G1-1 mg/kg, G2-5 mg/kg and G3-10 mg/kg, once a day for 15 days (d0 to d + 14). Blood samples were collected from the animals of the treated groups before and at d + 1, + 2, + 4, + 7, + 15 and + 21. The guinea pigs were artificially infested at d + 7 with A. sculptum larvae, and specimens were recovered at d + 11 to d + 14 and kept in a climatized chamber for 14 days. In Study II (evaluation of pharmacokinetic parameters), one group of eight animals received FLU administered by gavage in a single dose of 10 mg/kg, and blood samples were collected before and on day 0 (8 h after treatment), + 1, + 4, + 7, + 15, + 21 and + 28 after single FLU administration. FLU was analyzed in plasma samples by high-performance liquid chromatography with ultraviolet detection. Results: FLU plasma concentrations increased quickly, indicating rapid absorption, and decreased slowly. Some larvae from all treated groups exhibited morphological and behavioral changes. FLU interfered in molting, and the efficacy obtained was 100% for all treated groups. Conclusions: The results offer promising perspectives for the development of a palatable feed cube containing FLU for free-living capybaras to control A. sculptum and also to prevent BSF in areas where capybaras have been shown to play a primary role.
Resistance of the cattle tick Rhipicephalus (Boophilus) microplus to Fluazuron in Argentina
Exp Appl Acarol 2022 Apr;86(4):599-606.PMID:35503589DOI:10.1007/s10493-022-00713-y.
The aim of this work is to report the presence of resistance to Fluazuron in a population of Rhipicephalus microplus in Argentina. The evidence was obtained from field and in vitro trials. In the field trial, cattle infested with ticks was treated with two commercial formulations of Fluazuron. The in vitro trial (adult immersion test, AIT) was performed by using technical grade Fluazuron. In the field trial, there were no significant differences between the treated and control groups between days 2 and 34 post-treatment. The only exceptions (treated group I in day 14 post-treatment, treated group II in days 23 and 29 post-treatment) had a significantly lower tick load than the untreated group, but the efficacy was not higher than 70%. Viable engorged females were collected on both groups of treated bovines in all counts, and the production of viable larvae was not precluded with the application of the two commercial formulations of Fluazuron evaluated in this study. The results obtained with the in vitro assay (AIT) also indicate that the R. microplus population tested in this work has a higher level of resistance to Fluazuron than another susceptible field strain. The integrated analysis of the field and in vitro trials clearly reveals the emergence of resistance to Fluazuron in a R. microplus population from Argentina. This diagnosis of resistance does not imply that the Fluazuron has lost its functionality at a regional scale, but it highlights the need to establish control strategies that minimize the use of this drug in order to preserve its functionality as an acaricide.
Ecotoxicological assessment of Fluazuron: effects on Folsomia candida and Eisenia andrei
Environ Sci Pollut Res Int 2019 Feb;26(6):5842-5850.PMID:30613876DOI:10.1007/s11356-018-4022-7.
The cattle production in Brazil has increased considerably in the last years, mainly due to the control of parasite infestation of the animals, which cause loss of productivity to the sector. Fluazuron is an active ingredient (a.i.) of the benzoylurea class used to control ticks in cattle. As this a.i. has been found unchanged in animal feces, which may present a risk to edaphic organisms, this study aimed to assess the effects of Fluazuron on survival, reproduction, and behavior of the soil invertebrates Folsomia candida and Eisenia andrei, through ecotoxicological assays. We carried out bioassays in a tropical artificial soil (TAS) spiked with increasing doses of the insecticide. Earthworm mortality was found only at the highest tested Fluazuron concentration (LOEC = 160 mg a.i. kg-1 dry soil and NOEC = 80 mg kg-1), while the reproduction of F. candida and E. andrei was reduced at lower Fluazuron concentrations (EC50 = 4.48 mg kg-1 and EC50 = 20.8 mg kg-1, respectively). Avoidance behavior was detected for both species at lower concentrations than those that caused impacts on reproduction, indicating that the substance may affect the soil habitat function. Since the possible adverse effects of Fluazuron on edaphic fauna are still unknown or neglected, this study also warns about the possible harmful effect of veterinary pharmaceutical products on edaphic fauna.
Novel Acaricidal Drug Fluazuron Causes Immunotoxicity via Selective Depletion of Lymphocytes T CD8
Evid Based Complement Alternat Med 2019 May 7;2019:2815461.PMID:31205477DOI:10.1155/2019/2815461.
Fluazuron is one of the newest veterinary antitick medicines. Belonging to the benzoylphenylureas group, its mechanism of action acts by the interference of the formation of the chitin of the tick, which is responsible for the hardening of its exoskeletons. In addition to taking care of the health of the animal so that it receives the medication in the doses and the correct form, it is important to analyze the safety of the operator. Reduced resistance to infectious disease was a well-documented consequence of primary and acquired immunodeficiencies, but a novel finding following xenobiotic exposure. The awareness of the consequences of altered immune function is the most likely outcome of inadvertent exposure. The human health implications of studies in which chemical exposure reduced resistance to infection drove an early focus on immunosuppression within the toxicology community. The main objective is to perform the evaluation by computational platforms and in cell culture, searching for data that can serve as a foundation for a better understanding of the toxic effects involved with the accidental contamination of Fluazuron and, thus, to assist the medical community and users to understand the risks inherent in its use. As far as we can determine in the literature, our work has unmistakably demonstrated that the Fluazuron can cause genotoxicity by probable chromatin rearrangement and immunodepleting by specific reduction of the CD8 T lymphocyte subpopulation, mediated by the decrease in gamma interferon production. Although the use of Fluazuron is a necessity for tick control and for cattle management, we must bear in mind that the imminent risks to its application exist. Careless use can damage the immune system which in turn carries a gigantic hazard by opening a door to diseases and pathogens and leaving us defenseless.