Milbemycin oxime
(Synonyms: 米尔贝肟) 目录号 : GC32173
An insecticidal antibiotic
Cas No.:129496-10-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Milbemycin oxime is a semisynthetic macrocyclic lactone prepared by the oxidation and oximation of an 80:20 ratio of milbemycin A3 and A4 . Like other milbemycin/avermectins, it can potentiate glutamate and GABA-gated chloride-channel opening and is used as a nematocide and insecticide in veterinary medicine.1,2
1.Duke, S.O., Cantrell, C.L., Meepagala, K.M., et al.Natural toxins for use in pest managementToxins (Basel)2(8)1943-1962(2010) 2.Bienhoff, S.E., Kok, D.J., Roycroft, L.M., et al.Efficacy of a single oral administration of milbemycin oxime against natural infections of Ancylostoma braziliense in dogsVet. Parasitol.195(1-2)102-105(2013)
| Cas No. | 129496-10-2 | SDF | |
| 别名 | 米尔贝肟 | ||
| Canonical SMILES | CC1=C[C@@H]2[C@@]3(O)[C@H](OC/C3=C\C=C\[C@H](C)C/C(C)=C/C[C@@H](O[C@@]4(CC[C@H](C)[C@@H](C)O4)C5)C[C@@H]5OC2=O)/C1=N\O.CC6=C[C@@H]7[C@@]8(O)[C@H](OC/C8=C\C=C\[C@H](C)C/C(C)=C/C[C@@H](O[C@@]9(CC[C@H](C)[C@@H](CC)O9)C%10)C[C@@H]%10OC7=O)/C6=N\O | ||
| 分子式 | C63H88N2O14 | 分子量 | 1097.38 |
| 溶解度 | DMSO : ≥ 29 mg/mL (26.43 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 0.9113 mL | 4.5563 mL | 9.1126 mL |
| 5 mM | 0.1823 mL | 0.9113 mL | 1.8225 mL |
| 10 mM | 0.0911 mL | 0.4556 mL | 0.9113 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。
Efficacy of oral afoxolaner plus Milbemycin oxime chewables against induced gastrointestinal nematode infections in dogs
Vet Parasitol 2016 Jul 30;225:117-22.PMID:27369586DOI:10.1016/j.vetpar.2016.06.003.
The efficacy of oral afoxolaner plus Milbemycin oxime combination chewables against induced gastrointestinal nematode infections in dogs was evaluated in six separate studies. Two studies were performed to evaluate the efficacy of the product against Toxocara canis, two studies evaluated the efficacy against Toxascaris leonina, one study evaluated the efficacy against Ancylostoma braziliense, and one study evaluated the efficacy against Ancylostoma caninum. In the A. caninum study, the efficacy of Milbemycin oxime alone and afoxolaner alone was also evaluated. Dogs in all studies were inoculated with infective eggs or larvae and confirmed to have patent infections based on a fecal examination prior to allocation to study group and treatment. Each study utilized a randomized block design with blocks based on pre-treatment body weight. All dogs were assigned to blocks based on body weight, and then each dog within a block was randomly assigned to treatment group. There were two groups of 10 dogs each in the T. canis, T. leonina, and A. braziliense studies: 1) an untreated (control) group and 2) a group treated with afoxolaner plus Milbemycin oxime chewables (NexGard Spectra(庐), Merial). This group was treated at a dose as close as possible to the minimum effective dose of afoxolaner and Milbemycin oxime (2.5mg+0.5mg per kg body weight, respectively) once on Day 0 using whole chews. There were four groups of 10 dogs each in the A. caninum study: 1) untreated (control), 2) NexGard Spectra(庐) as described above, 3) Milbemycin oxime alone (dose of at least 0.5mg per kg of body weight) and 4) afoxalaner alone (dose of at least 2.5mg per kg body weight). For parasite recovery and counts, dogs were euthanized humanely and necropsied seven days after treatment. The efficacy of the afoxolaner plus Milbemycin oxime combination was 鈮?8% against T. canis, 鈮?5.8% against T. leonina, and 90.2% against A. braziliense. Efficacy of the combination against A. caninum was 99.7%, while the efficacy of Milbemycin oxime alone was 99.6% and the efficacy of afoxolaner alone was 2.1%. Dogs treated with afoxolaner plus Milbemycin oxime chewables had significantly (p鈮?.0002) fewer nematodes than the untreated controls in all studies. There were no adverse events or other health problems that were related to treatment with Nexgard Spectra(庐) in these studies. The results of these controlled studies demonstrate the high efficacy of the afoxolaner plus Milbemycin oxime chewables against a broad range of canine intestinal nematode infections.
The intravenous and oral pharmacokinetics of afoxolaner and Milbemycin oxime when used as a combination chewable parasiticide for dogs
J Vet Pharmacol Ther 2017 Jan;40(1):35-43.PMID:27604405DOI:10.1111/jvp.12332.
The pharmacokinetics of afoxolaner and Milbemycin oxime (A3 and A4 forms) in dogs were evaluated following the oral administration of NexGard Spectra庐 (Merial), a fixed combination chewable formulation of these two active pharmaceutical ingredients. Absorption of actives was rapid at levels that provide the minimum effective doses of 2.5 mg/kg and 0.5 mg/kg of afoxolaner and Milbemycin oxime, respectively. The time to maximum afoxolaner plasma concentrations (tmax ) was 2-4 h. The milbemycin tmax was 1-2 h. The terminal plasma half-life (t1/2 ) and the oral bioavailability were 14 卤 3 days and 88.3% for afoxolaner, 1.6 卤 0.4 days and 80.5% for Milbemycin oxime A3 and 3.3 卤 1.4 days and 65.1% for Milbemycin oxime A4. The volume of distribution (Vd ) and systemic clearance (Cls) were determined following an IV dose of afoxolaner or Milbemycin oxime. The Vd was 2.6 卤 0.6, 2.7 卤 0.4 and 2.6 卤 0.6 L/kg for afoxolaner, Milbemycin oxime A3 and Milbemycin oxime A4, respectively. The Cls was 5.0 卤 1.2, 75 卤 22 and 41 卤 12 mL/h/kg for afoxolaner, Milbemycin oxime A3 and Milbemycin oxime A4, respectively. The pharmacokinetic profile for the combination of afoxolaner and Milbemycin oxime supports the rapid onset and a sustained efficacy for afoxolaner against ectoparasites and the known endoparasitic activity of Milbemycin oxime.
Efficacy of Milbemycin oxime/afoxolaner chewable tablets (NEXGARD SPECTRA庐) against Capillaria aerophila and Capillaria boehmi in naturally infected dogs
Parasit Vectors 2021 Mar 6;14(1):143.PMID:33676579DOI:10.1186/s13071-021-04648-y.
Background: Capillaria aerophila and Capillaria boehmi parasitize the respiratory system of wild and domestic carnivores. Capillaria aerophila inhabits the trachea and bronchi of dogs and cats, while C. boehmi affects the nasal cavities and sinuses of dogs. In dogs the infection may be subclinical or characterized by varying respiratory distress. Methods: The present study evaluated the efficacy of an oral formulation containing Milbemycin oxime and afoxolaner (NEXGARD SPECTRA庐) in dogs naturally infected with C. aerophila and/or C. boehmi from three enzootic areas of Italy. Dogs were enrolled pending fecal examination and molecular confirmation of respiratory capillarioses. Dogs were allocated in two groups: Group 1 (G1, 25 dogs), treated with a negative control product with no anthelmintic activity (afoxolaner, NEXGARD庐), and Group 2 (G2, 26 dogs), treated with NEXGARD SPECTRA庐. At the day of treatment administration (Day 0), all dogs were clinically examined. Dogs were again subjected to clinical and fecal examinations at Days 28 (卤 4) and 56 (卤 2). The primary criterion for treatment efficacy was the reduction of fecal Capillaria egg counts in G2 compared with G1. The regression of/recovery from baseline clinical signs was considered as a further efficacy criterion. Results: Percentage reduction of fecal Capillaria egg counts in the NEXGARD SPECTRA庐 group compared to the control group was > 97% on Day 28 and 100% on Day 56, respectively (p < 0.05 for both time points). Twelve of the 13 dogs in the NEXGARD SPECTRA庐 group with respiratory signs prior to treatment were free of clinical signs at the end of the study. Conversely, the six control group dogs with respiratory signs prior to treatment remained symptomatic. Conclusions: Results of the present study showed that NEXGARD SPECTRA庐 was safe and highly efficacious in the reduction of C. aerophila and C. boehmi eggs after one treatment with a complete reduction of the egg output after the second administration associated with a recovery from respiratory signs.
Evaluation of compounded aqueous Milbemycin oxime: issues with formulation potency and reproducibility
J Small Anim Pract 2019 Jan;60(1):27-31.PMID:29998573DOI:10.1111/jsap.12907.
Objectives: To determine the potency and reproducibility of Milbemycin oxime when compounded as an aqueous suspension (20 mg/mL). Materials and methods: Preparation choice reflected current prescribing practices. Samples were acquired by prescription from two national veterinary compounding pharmacies at three time points. Two different storage conditions were evaluated and sampled at four time points from the order date (day 7, 14, 21 and 28). Milbemycin oxime recovery was performed by solid-phase extraction and concentration strength measured via high-performance liquid chromatography. Results: The average concentration on day 7 for Pharmacy A samples was 16.29 mg/mL [confidence interval (CI): 15.66 to 16.92] with a coefficient of variation (CV) = 11%, while for Pharmacy B it was 20.46 mg/mL (CI: 19.83 to 21.08) with CV = 22%. The mean decrease in concentration over 28 days for Pharmacy A was 22% (CI: 9% to 34%) while Pharmacy B was 18% (CI: 2% to 35%). Clinical significance: The compounded Milbemycin oxime suspensions evaluated in this study deviated by more than 10% from their labelled strength in five of the six lots. Clinical efficacy of compounded Milbemycin oxime suspensions remains unknown and the use of these products should be discouraged at this time.
Macrocyclic lactone resistance in Dirofilaria immitis: risks for prevention of heartworm disease
Int J Parasitol 2021 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.