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Dicyclanil

目录号 : GC25348

Dicyclanil is a pyrimidine-derived regulator of insect growth used for topical treatment of sheep to prevent larval infestation by the blowfly.

Dicyclanil Chemical Structure

Cas No.:112636-83-6

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25mg
¥556.00
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产品描述

Dicyclanil is a pyrimidine-derived regulator of insect growth used for topical treatment of sheep to prevent larval infestation by the blowfly.

Chemical Properties

Cas No. 112636-83-6 SDF Download SDF
分子式 C8H10N6 分子量 190.21
溶解度 DMSO: 38 mg/mL (199.78 mM);Water: Insoluble;Ethanol: 2 mg/mL (10.51 mM) 储存条件 Store at -20°C
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1 mM 5.2573 mL 26.2867 mL 52.5735 mL
5 mM 1.0515 mL 5.2573 mL 10.5147 mL
10 mM 0.5257 mL 2.6287 mL 5.2573 mL
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Research Update

Dicyclanil (Veterinary Medicinal Products)

Food Saf (Tokyo) 2018 Sep 28;6(3):136-138.PMID:32038901DOI:10.14252/foodsafetyfscj.2018007s.

Food Safety Commission of Japan (FSCJ) conducted a risk assessment of dicycranil (CAS No. 112636-83-6), a pyrimidine-derived insect growth regulator, using the evaluation reports from the Joint FAO/WHO Expert Committee on Food Additives (JECFA), the European Medicines Agency (EMEA), and also the Australian government. In an 18-month chronic toxicity/carcinogenicity study in mice, increased incidences of hepatocellular adenomas and carcinomas were observed in females in the 500 ppm group. In spite of a recent experiment implying the possible indirect genotoxicity of Dicyclanil on the carcinogenicity, Dicyclanil is unlikely to exert the carcinogenicity in vivo through the genotoxic mechanism judging from other studies. FSCJ recognized it as feasible to set the threshold value. Adverse effects detected at the lowest dose in various toxicological studies were the increased plasma levels of cholesterol and phospholipid at 100 ppm (equivalent to 2.7 mg/kg bw/day in males and 3.5 mg/kg bw/day in females) in a 90-day subacute toxicity study in dogs. No-observed-adverse-effect level (NOAEL) of this study was 20 ppm (equivalent to 0.61 mg/kg bw/day in males and 0.71 mg/kg bw/day in females). On the other hand, the NOAEL in a long term study, a 12-month chronic toxicity study in dogs was 25 ppm (equivalent to 0.71 mg/kg bw/day in males) based on increased level of plasma cholesterol observed only in males at 150 ppm (equivalent to 4.4 mg/kg bw/day in males and 5.1 mg/kg bw/day in females). The increased cholesterol levels in plasma were common in both studies in dogs. It was appropriate to choose the NOAEL for the effect on cholesterol in the longer term treatment, and thus FSCJ adopted the NOAEL of 0.71 mg/kg bw/day. Consequently, FSCJ specified the ADI of 0.0071 mg/kg bw/day for Dicyclanil based on the NOAEL of 0.71 mg/kg bw/day in the 12-month chronic toxicity study in dogs, by applying a safety factor of 100.

Resistance to Dicyclanil and imidacloprid in the sheep blowfly, Lucilia cuprina, in Australia

Pest Manag Sci 2022 Oct;78(10):4195-4206.PMID:35690912DOI:10.1002/ps.7037.

Background: The sheep blowfly, Lucila cuprina, is a myiasis-causing parasite responsible for significant production losses and welfare issues for the Australian sheep industry. Control relies largely on the use of insecticides. The pyrimidine compound, Dicyclanil, is the predominant control chemical, although other insecticides also are used, including imidacloprid, ivermectin, cyromazine and spinosad. We investigated in vitro resistance patterns and mechanisms in field-collected blowfly strains. Results: The Walgett 2019 strain showed significant levels of resistance to both Dicyclanil and imidacloprid, with resistance factors at the IC50 of 26- and 17-fold, respectively, in in vitro bioassays. Co-treatment with the cytochrome P450 inhibitor, aminobenzotriazole, resulted in significant levels of synergism for Dicyclanil and imidacloprid (synergism ratios of 7.2- and 6.1-fold, respectively), implicating cytochrome P450 in resistance to both insecticides. Cyp12d1 transcription levels were increased up to 40-fold throughout the larval life stages in the resistant strain compared to a reference susceptible strain, whereas transcription levels of some other cyp genes (6g1, 4d1, 28d1) did not differ between the strains. Similar resistance levels also were observed in flies collected from the same property in two subsequent years. Conclusion: This study indicates that in vitro resistance to both Dicyclanil and imidacloprid in this field-collected blowfly strain is likely mediated by cytochrome P450, with Cyp12d1 implicated as the enzyme responsible; however, it remains possible that another P450 also may be involved. A common resistance mechanism for the two drugs has important implications for drug rotation strategies designed to prolong the useful life of flystrike control chemicals. © 2022 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Dicyclanil resistance in the Australian sheep blowfly, Lucilia cuprina, substantially reduces flystrike protection by Dicyclanil and cyromazine based products

Int J Parasitol Drugs Drug Resist 2020 Dec;14:118-125.PMID:33035968DOI:10.1016/j.ijpddr.2020.04.005.

Late in 2017, field samples of the Australian sheep blowfly, Lucilia cuprina, were submitted by sheep producers from three states of Australia (South Australia, Victoria and New South Wales). Some were collected by submitters concerned about shortened periods of flystrike protection from Dicyclanil based products. Neonate larval offspring from the NSW field samples survived and successfully completed their life cycles following exposure to Dicyclanil and cyromazine at susceptible discriminating concentrations in vitro. The in vivo study reported here used Dicyclanil resistant neonate larvae to assess the flystrike protection provided by a cyromazine jetting fluid and a number of Dicyclanil based spray-on products, when applied to sheep six weeks after shearing. The two Dicyclanil resistant blowfly strains used in this study showed in vitro resistance ratios, at the LC50, of approximately 13- and 25-fold relative to a Dicyclanil and cyromazine susceptible strain. Compared to the levels of resistance that L. cuprina has developed to other insecticides these are relatively low, however, three Dicyclanil based spray-on products (active ingredient 12.5 g/L, 50 g/L and 65 g/L) had protection periods reduced by 73%, 78% and 69% respectively when compared to the maximum protection periods claimed by the manufacturer. A 50% and a 33% reduction in protection period was also observed to a cyromazine and an ivermectin based jetting fluid respectively. In contrast, protection periods were attained or exceeded regardless of the treatment used against field derived Dicyclanil susceptible neonate larvae. For the first time we confirm that Dicyclanil resistance enables the completion of the L. cuprina life cycle following flystrike initiation on Dicyclanil or cyromazine treated sheep when insecticide levels are considered high and protective. This study also provides in vivo information on the effect of Dicyclanil resistance on the protection provided by a product with an active ingredient belonging to an unrelated insecticide group. Dicyclanil resistance is of major concern to the Australian sheep industry.

Field trial of the efficacy of Dicyclanil for the prevention of wohlfahrtiosis of sheep

Vet Rec 2005 Jan 8;156(2):37-40.PMID:15675521DOI:10.1136/vr.156.2.37.

Two groups of 40 ewes from each of two flocks were used in a field trial of the efficacy of Dicyclanil to protect them against a natural infestation by Wohlfahrtia magnifica larvae, when administered topically as a spray-on formulation. The animals of one group in each flock were treated with Dicyclanil and those of the other group were left untreated as controls. The trial lasted 31 weeks and the animals were inspected daily for wohlfahrtiosis. The incidences of wohlfahrtiosis ranged from 17.5 per cent to 20 per cent in the control groups and from 2.5 per cent to 5 per cent in the treated groups, and 77.8 per cent of the infestations were in the genitalia. When compared with the control groups, Dicyclanil achieved a 100 per cent reduction of infestation in the treated groups of both flocks for at least 24 weeks, and an 80 per cent reduction for 31 weeks.

Strategic use of crutching and Dicyclanil to protect unmulesed sheep against breech strike

Aust Vet J 2009 Apr;87(4):138-41.PMID:19335467DOI:10.1111/j.1751-0813.2009.00408.x.

Objective: To test strategies for the application of Dicyclanil and mid-season crutching to maximise protection of unmulesed sheep against breech strike. Procedure: Three hundred and eighty unmulesed Merino weaners were randomly allocated to four groups either left untreated or treated by different strategies with 50 g/L Dicyclanil. Treatments included breech treatment alone and breech plus body treatment, with two application times, immediately after shearing and 6 weeks after crutching or shearing. To assess protection, larval implants with newly hatched Lucilia cuprina larvae were applied to 10 different sheep from each group at 3, 4, 5 and 6 months after crutching and shearing and assessed for the development of strike at 48 hours. The concentration of Dicyclanil was measured in wool samples clipped from the breeches of the test sheep. Results: All Dicyclanil treatments gave significant reduction in strike in comparison to controls up until 4 months after crutching but protection in the sheep treated immediately after shearing had waned at 5 months. Treating at 6 weeks after crutching provided significant reduction (P < 0.05) in strike for 6 months. Results for strike incidence immediately after shearing and concentration of Dicyclanil in the breech wool also suggested improvements in protection by delaying treatment for 6 weeks. Conclusion: In most environments it should be possible to protect unmulesed sheep against breech strike with a carefully planned integrated control program incorporating strategically timed crutching, shearing and Dicyclanil application. Delaying treatment with Dicyclanil to at least 6 weeks after shearing or crutching increased the protection provided in comparison to treatment immediately after shearing.