Spirodiclofen (BAJ-2740)
(Synonyms: 螺螨酯; BAJ-2740) 目录号 : GC33967
Spirodiclofen (BAJ-2740) 是一种广谱杀螨剂，通过抑制脂质生物合成 (LBI) 发挥作用，对目前可用的杀螨剂没有交叉耐药性，并具有额外的杀虫特性。
Cas No.:148477-71-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Spirodiclofen is a broad spectrum acaricide acting via lipid biosynthesis inhibition (LBI) with no cross resistance to currently available acaricides and with additional insecticidal properties.
[1]. De Maeyer L, et al. The multiple target use of spirodiclofen (Envidor 240 SC) in IPM pomefruit in Belgium. Commun Agric Appl Biol Sci. 2009;74(1):225-232.
| Cas No. | 148477-71-8 | SDF | |
| 别名 | 螺螨酯; BAJ-2740 | ||
| Canonical SMILES | CCC(C)(C)C(OC1=C(C2=CC=C(Cl)C=C2Cl)C(OC13CCCCC3)=O)=O | ||
| 分子式 | C21H24Cl2O4 | 分子量 | 411.32 |
| 溶解度 | DMSO : ≥ 28 mg/mL (68.07 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 | 2.4312 mL | 12.156 mL | 24.312 mL |
| 5 mM | 0.4862 mL | 2.4312 mL | 4.8624 mL |
| 10 mM | 0.2431 mL | 1.2156 mL | 2.4312 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。
Molecular docking and toxicity assessment of Spirodiclofen: protective role of lycopene
Environ Sci Pollut Res Int 2021 Oct;28(40):57372-57385.PMID:34091852DOI:10.1007/s11356-021-14748-y.
In this study, toxic effects of Spirodiclofen and protective role of lycopene against toxic effects were investigated by using physiological, cytogenetic, anatomical, and biochemical parameters. Allium cepa L. bulbs were used as test material. The bulbs were divided into six groups as one control and five application groups. Bulb in the control group was germinated with tap water, and in treatment groups, 20-mg L-1 dose of Spirodiclofen 215- and 430-mg L-1 doses of lycopene were applied. Spirodiclofen application caused a decrease in physiological parameters such as germination percentage, root length, and weight increase. Spirodiclofen administration caused a decrease in the percentage of mitotic index (MI) and an increase in DNA fragmentation, micronucleus (MN), and chromosomal aberration (CA) frequency. Spirodiclofen application caused an increase in the level of the oxidant compound malondialdehyde (MDA), changes in the level of antioxidant enzymes, and disruption of the oxidant/antioxidant balance in the cell. Molecular interactions between Spirodiclofen and antioxidant enzymes were determined by molecular docking analysis. In addition to physiological, biochemical, and genetic abnormalities, Spirodiclofen also caused deformations in the anatomy of the A. cepa root tip meristematic cells. Lycopene treatment showed a protective effect by suppressing the toxic effects of Spirodiclofen, causing a significant improvement in the values of selected physiological, cytogenetic, anatomical, and biochemical parameters. As a result, Spirodiclofen insecticide caused toxic effects on various parameters in A. cepa, which is a eukaryotic model organism. In order to elucidate the toxicity mechanism, each parameter is associated with each other. Molecular docking method has revealed the effects of Spirodiclofen on antioxidant enzymes. Lycopene application together with Spirodiclofen resulted in the regression of all toxic effects and improvement in the root tissue. This result shows that lycopene has a strong protective property against Spirodiclofen toxicity.
Biochemical and Molecular Analysis of Field Resistance to Spirodiclofen in Panonychus citri (McGregor)
Insects 2022 Nov 2;13(11):1011.PMID:36354837DOI:10.3390/insects13111011.
Spirodiclofen is one of the most widely used acaricides in China. The citrus red mite, Panonychus citri (McGregor) (Acari: Tetranychidae), is one of the most destructive citrus pests worldwide and has developed a high resistance to Spirodiclofen. However, the molecular mechanism of Spirodiclofen resistance in P. citri is still unknown. In this study, we identified a field spirodiclofen-resistant strain (DL-SC) that showed 712-fold resistance to Spirodiclofen by egg bioassay compared to the susceptible strain. Target-site resistance was not detected as non-synonymous mutations were not found by amplification and sequencing of the ACCase gene of resistant and susceptible strains; in addition, the mRNA expression levels of ACCase were similar in both resistant and susceptible strains. The activity of detoxifying enzymes P450s and CCEs in the resistant strain was significantly higher than in the susceptible strain. The transcriptome expression data showed 19 xenobiotic metabolisms genes that were upregulated. Stage-specific expression profiling revealed that the most prominent upregulated gene, CYP385C10, in transcriptome data was significantly higher in resistant strains in all stages. Furthermore, functional analysis by RNAi indicated that the mortality caused by Spirodiclofen was significantly increased by silencing the P450 gene CYP385C10. The current results suggest that overexpression of the P450 gene, CYP385C10, may be involved in Spirodiclofen resistance in P. citri.
Residue level, persistence and safety of spirodiclofen-pyridaben mixture in citrus fruits
Food Chem 2016 Mar 1;194:805-10.PMID:26471621DOI:10.1016/j.foodchem.2015.08.044.
A sample pretreatment method was established to analyze the residues of spirodiclofen-pyridaben mixture in citrus fruits using ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS). A mixed formulation of 27% spirodiclofen-pyridaben suspension concentrates was sprayed on citrus in field conditions at 1- or 1.5-fold recommended dose. The dissipation of spirodiclofen-pyridaben mixture in whole citrus follows the first-order dynamic equation with half-lives of 4.56-13.1d at three locations. Residues of spirodiclofen-pyridaben mixture are mainly distributed in peel, followed by whole citrus and pulp. Risk assessment showed that Spirodiclofen exerts much higher chronic risk than acute risk, while pyridaben exerts relatively lower chronic risk than acute risk. However, both chronic and acute risks of this mixed pesticide in citrus fruits are relatively low to humans irrespective of dosages, frequency of applications, and pre-harvest intervals. The residue dynamics information will support label-claim for use of this mixed pesticide in citrus fruits.
[Dissipation dynamics of Spirodiclofen in wolfberry fruit]
Zhongguo Zhong Yao Za Zhi 2016 Jun;41(12):2190-2193.PMID:28901058DOI:10.4268/cjcmm20161203.
The dissipation of Spirodiclofen in fresh fruit and dry fruit of wolfberry was detected in this study to provide a reference for its safe application.According to Pesticide Residue Test Criteria of China, the open-field experiment was conducted in Zhongning courty of Ningxia province, and the dissipation of Spirodiclofen was studied by acetonitrile extraction and HPLC-MS/MS detection. The results showed that the half-lives of Spirodiclofen in fresh wolfberry fruit and dry wolfberry fruit were 6.9-11.2 days and 8.5-10.4 days, respectively. Spirodiclofen belongs to the easily degradable pesticide type. According to the maximum residue limits (0.5 mg•kg⁻¹) of Spirodiclofen of EU for wolfberry, after recommended dosage being sprayed for once, fresh wolfberry fruit was safe to eat after 5 days, and dry wolfberry fruit was safe to eat after 21 days.
The role of detoxification enzymes in the susceptibility of Brevipalpus californicus exposed to acaricide and insecticide mixtures
Pestic Biochem Physiol 2021 Jun;175:104855.PMID:33993973DOI:10.1016/j.pestbp.2021.104855.
The intense spraying of pesticides to control different arthropod pests has resulted in negative side effects for the management of pests. It was previously discovered that exposure to non-acaricidal insecticides alone or in a mixture, results in lower efficiency of the acaricide Spirodiclofen used for Brevipalpus spp. control. We investigate here whether the induced expression of detoxification enzymes by non-lethal insecticides may antagonize Spirodiclofen toxicity. Brevipalpus californicus mites exposed to the insecticide phosmet alone or in combination with Spirodiclofen showed increased activity of P450 monooxygenases (P450s). No antagonistic effects in mite mortality were observed by the combination of phosmet and Spirodiclofen. On the other hand, mites exposed to the insecticide imidacloprid alone or in combination with Spirodiclofen showed an increase in the activity of P450s, carboxylcholinesterases (CCE), and glutathione-S-transferases (GST). An antagonistic effect on mite mortality was observed when mites were exposed to the LC25 of Spirodiclofen combined with the field rate treatment of imidacloprid. The addition of PBO (a P450 monooxygenase inhibitor) to the mixture of Spirodiclofen and imidacloprid resulted in a synergistic effect over mite mortality but the addition of DEM (a GST inhibitor) resulted in an antagonist effect. Taken together, this study showed that the combination of imidacloprid with Spirodiclofen is antagonistic for the control of B. californicus, and this results from the induction of detoxification enzymes, such as P450s, CCE, and GST. The use of inhibitors highlights the role of these enzymes in the antagonism of the mixture.