Milbemectin
(Synonyms: Milbemycin A3 (~30%) and Milbemycin A4 (~70%) Mixture) 目录号 : GC47676
An insecticidal antibiotic
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Milbemectin is an insecticide used primarily to control mites.1 Milbemectin is a mixture of milbemycin A3 and milbemycin A4 that has acaricidal and nematocidal activity against adult spider mites, spider mite eggs, and C. elegans with IC50 values of 5.3, 41.1, and 9.5 µg/ml, respectively.2 It acts as an allosteric agonist of the Drosophila RDL GABA receptor.3 It is also effective against the pinewood nematode, B. xylophilus with an LC20 of 0.0781 mg/liter.4
1.Macrocyclic InsecticidesMetabolic Pathways of Agrochemicals, Part 2: Insecticides and Fungicides (Metabolic Pathways)95-98(1999) 2.Yang, L.Y., Wang, J.D., Zhang, J., et al.New nemadectin congeners with acaricidal and nematocidal activity from Streptomyces microflavus neau3 Y-3Bioorg. Med. Chem. Lett.23(20)5710-5713(2013) 3.Nakao, T., Banba, S., and Hirase, K.Comparison between the modes of action of novel meta-diamide and macrocyclic lactone insecticides on the RDL GABA receptor.Pestic. Biochem. Physiol.120101-108(2015) 4.Bi, Z., Gong, Y., Huang, X., et al.Efficacy of four nematicides against the reproduction and development of pinewood nematode, Bursaphelenchus xylophilus.J. Nematol.47(2)126-132(2015)
| Cas No. | N/A | SDF | |
| 别名 | Milbemycin A3 (~30%) and Milbemycin A4 (~70%) Mixture | ||
| Canonical SMILES | C/C(C[C@@H](C)/C=C/C=C(CO1)/[C@@]([C@@]1([H])[C@H](O)C(C)=C2)(O)[C@]2([H])C3=O)=C\C[C@]4([H])C[C@@](O3)([H])C[C@@]5(O[C@]([H])(C)[C@@H](C)CC5)O4.C/C(C[C@@H](C)/C=C/C=C(CO6)/[C@@]([C@@]6([H])[C@H](O)C(C)=C7)(O)[C@]7([H])C8=O)=C\C[C@]9([H])C[C@@](O8)([H])C[C@@]%10(O[C@]([H])(CC)[C@@H](C)CC%10)O9 | ||
| 分子式 | C31H44O7 (A3) and C32H46O7 (A4) | 分子量 | 0 |
| 溶解度 | DMF: Soluble,DMSO: Soluble,Ethanol: Soluble,Methanol: Soluble | 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。 | ||
| 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。
Milbemectin resistance in Tetranychus urticae (Acari: Tetranychidae): selection, stability and cross-resistance to abamectin
Exp Appl Acarol 2010 Mar;50(3):231-41.PMID:19760100DOI:10.1007/s10493-009-9304-9.
Studies on artificial laboratory selections with Milbemectin, stability of Milbemectin resistance and possible cross-resistance with abamectin were carried out with Tetranychus urticae Koch to provide basic information for a Milbemectin resistance management program. Selections for resistance and susceptibility to Milbemectin were performed in a population of T. urticae, collected from a commercial chrysanthemum field in the State of São Paulo, Brazil. After six selections for resistance and five selections for susceptibility, susceptible (S) and resistant (R) strains of T. urticae to Milbemectin were obtained. The resistance ratio (R/S) at the LC(50) reached 409-fold value. The stability of Milbemectin resistance was also studied under laboratory conditions, using a population with initial frequency of 75% of resistant mites. The frequencies of Milbemectin resistance were evaluated monthly for a period of 7 months. In order to observe possible correlation between Milbemectin and abamectin resistance, the frequencies of abamectin resistance were also evaluated for that population, during the same period. The frequency of Milbemectin resistance decreased from 75 to 14.5%, while the percentage of abamectin resistant mites decreased from 57 to 9.1%, in 7 months. The frequencies of Milbemectin and abamectin resistance were also evaluated in 25 field populations of T. urticae, collected from several crops in the State of São Paulo. The frequencies of Milbemectin resistance varied from 4.1 to 89.5%, and of abamectin, from 7.0 to 90.5%. A positive and significant correlation was observed between the frequencies of Milbemectin and abamectin resistance, indicating positive cross-resistance between these acaricides. The results indicate that abamectin should be avoided for managing Milbemectin resistance in T. urticae. This is the first report on Milbemectin resistance in T. urticae in Brazil.
Geographical distribution and molecular insights into abamectin and Milbemectin cross-resistance in European field populations of Tetranychus urticae
Pest Manag Sci 2020 Aug;76(8):2569-2581.PMID:32237053DOI:10.1002/ps.5831.
Background: Milbemectin and abamectin are frequently used to control the spider mite Tetranychus urticae. The development of abamectin resistance in this major pest has become an increasing problem worldwide, potentially compromising the use of Milbemectin. In this study, a large collection of European field populations was screened for Milbemectin and abamectin resistance, and both target-site and metabolic (cross-)resistance mechanisms were investigated. Results: High to very high levels of abamectin resistance were found in one third of all populations, while Milbemectin resistance levels were low for most populations. The occurrence of well-known target-site resistance mutations in glutamate-gated chloride channels (G314D in GluCl1 and G326E in GluCl3) was documented in the most resistant populations. However, a new mutation, I321T in GluCl3, was also uncovered in three resistant populations, while a V327G and L329F mutation was found in GluCl3 of one resistant population. A differential gene-expression analysis revealed the overexpression of detoxification genes, more specifically cytochrome P450 monooxygenase (P450) and UDP-glycosyltransferase (UGT) genes. Multiple UGTs were functionally expressed, and their capability to glycosylate abamectin and Milbemectin, was tested and confirmed. Conclusions: We found a clear correlation between abamectin and Milbemectin resistance in European T. urticae populations, but as Milbemectin resistance levels were low, the observed cross-resistance is probably not of operational importance. The presence of target-site resistance mutations in GluCl genes was confirmed in most but not all resistant populations. Gene-expression analysis and functional characterization of P450s and UGTs suggests that also metabolic abamectin resistance mechanisms are common in European T. urticae populations. © 2020 Society of Chemical Industry.
Sustainable chromatographic purification of Milbemectin: Application of high-speed countercurrent chromatography coupled with off-line atmospheric pressure solid analysis probe-high resolution mass spectrometry
J Chromatogr A 2023 Apr 12;1694:463901.PMID:36889118DOI:10.1016/j.chroma.2023.463901.
Isolation of valuable chemicals is an important process in reagent manufacturing for the pharmaceutical and food science industries. This process is traditionally time-consuming, expensive, and consumes vast amounts of organic solvents. Considering green chemistry and sustainability concerns, we sought to develop a sustainable chromatographic purification methodology for obtaining antibiotics by focusing on the reduction of organic solvent waste generation. Milbemectin (mixture of milbemycin A3 and milbemycin A4) was successfully purified using high-speed countercurrent chromatography (HSCCC) and pure fractions (>98% purity, HPLC) could be identified using the organic solvent fee atmospheric pressure solid analysis probe mass spectrometry (ASAP-MS). The organic solvents required for HSCCC could be redistilled and recycled for continued HSCCC purification, thus reducing the consumption of organic solvent (n-hexane/ethyl acetate) by 80+%. Optimization of the two-phase solvent system (n-hexane/ethyl acetate/methanol/water, 9/1/7/3, v/v/v/v) for HSCCC was assisted computationally, thereby reducing solvent waste from an experimental determination. Our proposal application of HSCCC and offline ASAP-MS provides proof of concept for a sustainable, preparative scale, chromatographic purification methodology for obtaining antibiotics in high purity.
Development and validation of an HPLC-FLD method for Milbemectin quantification in dog plasma
J Chromatogr B Analyt Technol Biomed Life Sci 2010 Jul 15;878(22):2013-7.PMID:20573552DOI:10.1016/j.jchromb.2010.05.037.
Milbemectin is a widely used veterinary antiparasitic agent. A high-performance liquid chromatography with fluorescent detection (HPLC-FLD) method is described for the determination of Milbemectin in dog plasma. The derivative procedure included mixing 1-methylimizole [MI, MI-ACN (1:1, v/v), 100 microL], trifluoroacetic anhydride [TFAA, TFAA-ACN (1:2, v/v), 150 microL] with a subsequent incubation for 3s at the room temperature to obtain a fluorescent derivative, which is reproducible in different blood samples and the derivatives proved to be stable for at least 80 h at room temperature. HPLC method was developed on C18 column with FLD detection at an excitation wavelength of 365 nm and emission wavelength of 475 nm, with the mobile phase consisting of methanol and water in the ratio of 98:2 (v/v). The assay lower limit of quantification was 1 ng/mL. The calibration curve was linear over concentration range of 1-200 ng/mL. The intra- and inter-day accuracy was >94% and precision expressed as % coefficient of variation was <5%. This method is specific, simple, accurate, precise and easily adaptable to measure milbemycin in blood of other animals.
Baseline susceptibility of persea mite (Acari: Tetranychidae) to abamectin and Milbemectin in avocado groves in Southern California
Exp Appl Acarol 2005;36(1-2):51-9.PMID:16082923DOI:10.1007/s10493-005-1545-7.
Persea mite, Oligonychus perseae Tuttle, Baker, and Abatiello, susceptibility to abamectin and Milbemectin was evaluated in 2003 to determine baseline susceptibility levels in avocado groves in San Diego and Ventura Counties (California, USA) where more than 70% of the state's avocado production is concentrated. Milbemectin has yet to be used in avocado production in California and abamectin has been available for use since 1999. Baseline susceptibility ratios (in relation to the most susceptible population) of five persea mite field strains to Milbemectin varied 2.1- to 2.8-fold at the LC50 and LC90, respectively. The susceptibility of seven field strains to abamectin varied slightly more (2.1- to 3.5-fold) with one strain subjected to seven sprays over the past 4 years showing slight but significant separation of LC50 and LC90's from the most susceptible strain, which is suggestive of the early stages of resistance to this product. Based on these data, baseline susceptibility levels are proposed that might be used to monitor for future persea mite resistance to these chemicals as their use in California avocado production continues.