Eprinomectin (MK-397)
(Synonyms: 依普菌素; MK-397) 目录号 : GC32117
An avermectin with anthelmintic and insecticidal activities
Cas No.:123997-26-2
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
Eprinomectin is an avermectin with anthelmintic and insecticidal activities.1 It is comprised of eprinomectin B1a and eprinomectin B1b .2 Eprinomectin (≥0.08 mg/kg, applied topically) reduces worm burden by 99% or more in bovine models of adult H. placei, O. ostertagi, T. axei, Cooperia punctata, N. helvetianus, O. radiatum, or D. viviparus infection.1 It also reduces parasite burden in bovine models of horn fly (H. irritans) or mange mite (C. bovis) infestation, as well as in cows naturally infested with lice (L. vituli), when applied topically at doses ranging from 0.16 to 0.5 mg/kg. Formulations containing eprinomectin have been used in the treatment and control of a variety of endo- and ectoparasites in cattle.
1.Shoop, W.L., Egerton, J.R., Eary, C.H., et al.Eprinomectin: A novel avermectin for use as a topical endectocide for cattleInt. J. Parasitol.26(11)1237-1242(1996) 2.Jiang, X., Hao, H.X., Growney, J.D., et al.Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal adenocarcinomaProc. Natl. Acad. Sci. USA110(31)12649-12654(2013)
| Cas No. | 123997-26-2 | SDF | |
| 别名 | 依普菌素; MK-397 | ||
| Canonical SMILES | C[C@H]1[C@@H](NC(C)=O)[C@@H](OC)C[C@H](O[C@@H]2[C@H](C)O[C@@H](O[C@@H](/C(C)=C/C[C@@H](C3)OC4(O[C@@H]([C@@H](CC)C)[C@H](C)C=C4)C[C@H]3OC5=O)[C@@H](/C=C/C=C6CO[C@@H]7[C@@]\6(O)[C@H]5C=C(C)[C@H]7O)C)C[C@@H]2OC)O1 | ||
| 分子式 | C50H75NO14 | 分子量 | 914.13 |
| 溶解度 | DMSO : ≥ 46 mg/mL (50.32 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 | 1.0939 mL | 5.4697 mL | 10.9394 mL |
| 5 mM | 0.2188 mL | 1.0939 mL | 2.1879 mL |
| 10 mM | 0.1094 mL | 0.547 mL | 1.0939 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。
Assessment of Avermectins-Induced Toxicity in Animals
Pharmaceuticals (Basel)2022 Mar 9;15(3):332.PMID:35337129DOI:10.3390/ph15030332.
Macrocyclic lactones, particularly the avermectins, have completely revolutionized the approaches aimed at control of parasites. These avermectins are the most widely used anti-parasitic drugs in veterinary field with sales exceeding one billion US dollars annually. However, before clinical usage, their safety evaluation in the animals is a major critical factor that must be considered. Many studies have reported the negative effects of avermectins like ivermectin, abamectin, doramectin, and Eprinomectin on the host animals. These harmful effects arise from avermectins targeting GABA and glutamate-gated chloride channels present both in the parasites and the host animals. In this review, various modes of avermectins action along with the negative effects on the host like nephrotoxicity, hepatotoxicity, neurotoxicity, reproductive toxicity, and endocrine disruption were discussed in detail. Furthermore, other important issues like ecotoxicity, drug resistance, and drug residues in milk associated with avermectins usage were also discussed, which need special attention.
Macrocyclic lactone resistance in Dirofilaria immitis: risks for prevention of heartworm disease
Int J Parasitol2021 Dec;51(13-14):1121-1132.PMID:34717929DOI:10.1016/j.ijpara.2021.08.006.
Heartworm disease, caused by Dirofilaria immitis, can be lethal in dogs and cats. It is transmitted by mosquitoes, and occurs in many parts of the world. Prevention relies on macrocyclic lactones. Macrocyclic lactones used are ivermectin, selamectin, abamectin, Eprinomectin, milbemycin oxime and moxidectin, administered at 30-day intervals during the transmission season. Some moxidectin formulations are long-acting injectables. In the USA, preventives are recommended throughout the year. Loss of efficacy of macrocyclic lactone preventives was reported in 2005 and proof of resistance in the USA was published a decade later. Understanding factors which promote resistance is important to maintain control. Factors important for resistance development are discussed. Better, inexpensive tests to confirm resistance are needed. Infection in animals under chemoprophylaxis per se does not imply resistance because lack of compliance in preventive use could be the reason. In vivo confirmation of resistance is expensive, slow and ethically questionable. A microfilariae suppression test can be a surrogate test, but requires a high dose of a macrocyclic lactone and repeated blood microfilaria counts 2-4 weeks later. DNA single nucleotide polymorphism markers have been successfully used. However, the specific genetic changes which cause resistance are unknown. Surveys to map and follow the extent of resistance are needed. Long acting mosquito repellants and insecticides can play a useful role. High dose rate formulations of moxidectin, coupled with mosquito biting mitigation may reduce transmission of resistant genotypes. Doxycycline, daily for 28 days, as anti-Wolbachia treatment, can reduce transmission and remove adult parasites. However, new classes of heartworm preventives are needed. While any preventive strategy must be highly effective, registration requirements for 100% efficacy may hinder development of useful new classes of preventives. Continued reliance on macrocyclic lactone preventives, when they do not work against resistant genotypes, will spread resistance, and allow for more disease.
Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects
Pharmaceuticals (Basel)2020 Aug 17;13(8):196.PMID:32824399DOI:10.3390/ph13080196.
Avermectins are a group of drugs that occurs naturally as a product of fermenting Streptomyces avermitilis, an actinomycetes, isolated from the soil. Eight different structures, including ivermectin, abamectin, doramectin, Eprinomectin, moxidectin, and selamectin, were isolated and divided into four major components (A1a, A2a, B1a and B2a) and four minor components (A1b, A2b, B1b, and B2b). Avermectins are generally used as a pesticide for the treatment of pests and parasitic worms as a result of their anthelmintic and insecticidal properties. Additionally, they possess anticancer, anti-diabetic, antiviral, antifungal, and are used for treatment of several metabolic disorders. Avermectin generally works by preventing the transmission of electrical impulse in the muscle and nerves of invertebrates, by amplifying the glutamate effects on the invertebrates-specific gated chloride channel. Avermectin has unwanted effects or reactions, especially when administered indiscriminately, which include respiratory failure, hypotension, and coma. The current review examines the mechanism of actions, biosynthesis, safety, pharmacokinetics, biological toxicity and activities of avermectins.
Efficacy of a pour-on formulation of Eprinomectin (MK-397) against nematode parasites of cattle, with emphasis on inhibited early fourth-stage larvae of Ostertagia spp
Am J Vet Res1997 Apr;58(4):379-83.PMID:9099383doi
Objective: To evaluate efficacy of topically applied eprinomectin against inhibited early fourth-stage larvae (IL4) of Ostertagia spp in calves. Animals: 4 groups (n = 6 [replicates]) for dose titration; 2 groups (n = 8 calves [replicates]) for dose confirmation. Procedure: 2 dose titration studies-0, 125, 250, and 500 micrograms of eprinomectin/kg of body weight-Louisiana and Georgia- and 2 dose confirmation studies of selected therapeutic dosage (500 micrograms/kg) in Scotland and France. Monitor calves were used to determine inhibition percentage of Ostertagia IL4. Test calves were ranked by weight in replicates of 4 (titration trials) or 2 (confirmation trials) animals each, and within replicates, were randomly allocated to treatment groups. Drug treatments were done on day 0, and animals were euthanatized by replicate, with holding time between treatment and euthanasia varying among trials from 14 to 27 days. Results: Observations indicated high efficacy (> 99%) of 500 micrograms of eprinomectin/kg in removal of Ostertagia IL4. Ostertagia and Cooperia were only genera common across sites, with efficacy of aforementioned dosage against adult and larval stages of both genera consistently high (> 99%). Results of 1 or both titration studies (500 micrograms/kg) indicated > 99 to 100% efficacy against adult Haemonchus placei, Trichostrongylus axei, T colubriformis, Bunostomum phlebotomum, Dictyocaulus viviparus, and Oesophagostomum radiatum. Lower efficacy values were observed at minimal (125 micrograms/kg) dosage. In France, 500 micrograms/kg was 85% effective against Trichostrongylus spp adults; however, numbers of control calves infected with Trichostrongylus spp and degree of infection were low. Adverse reactions were not evident. Conclusion: Eprinomectin given topically (500 micrograms) was highly effective against Ostertagia IL4 and other common nematodes of cattle.
Review of the Eprinomectin effective doses required for dairy goats: Where do we go from here?
Vet Parasitol2020 Jan;277:108992.PMID:31835054DOI:10.1016/j.vetpar.2019.108992.
Eprinomectin (EPM) has been recently granted a marketing authorisation in the European Union for use in goats, with a zero-day milk withdrawal period. Considering the high prevalence of benzimidazole resistance worldwide and the economic implications of managing milk residues, EPM may today be considered the main (or even the only) affordable treatment option, at least in dairy goats in the EU. However, the chosen dose (1 mg/kg) seems to be suboptimal, especially for lactating goats, and the chosen route of administration (Pour-on) highly subject to inter-individual variability. Considering the scarcity of anthelmintic resources, such a dosage regimen might threat the sustainability of this crucial drug in goat milk production and needs to be urgently discussed and reassessed.