Spinosad
(Synonyms: LY232105, XDE-105) 目录号 : GC48092
A naturally-occurring insecticide
Cas No.:168316-95-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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Spinosad is a naturally-occurring insecticide found in the the soil bacterium S. spinosa.1 It is a mixture of the macrocyclic lactones spinosyn A and spinosyn D , which act as agonists of insect nicotinic acetylcholinesterase receptors (nAChRs). Oral administration of spinosad induces toxicity in fruit flies including C. capitata, B. curcurbitae, and B. dorsalis (LC50s = 2.8-4.2, 4.3-5.5, and 3.1-3.3 µg/ml, respectively) but has low toxicity in vertebrates.2,3,4 It also inhibits canine P-glycoprotein (P-gp; IC50 = 0.2 µg/ml).5 Formulations containing spinosad have been used in the agricultural and veterinary control of insects.
1.Vo, D.T., Hsu, W.H., Abu-Basha, E.A., et al.Insect nicotinic acetylcholine receptor agonists as flea adulticides in small animalsJ. Vet. Pharmacol. Ther.33(4)315-322(2010) 2.Stark, J.D., Vargas, R., and Miller, N.Toxicity of spinosad in protein bait to three economically important tephritid fruit fly species (Diptera: Tephritidae) and their parasitoids (Hymenoptera: Braconidae).J. Econ. Entomol.97(3)911-915(2004) 3.SÁnchez-Bayo, F.Insecticides mode of action in relation to their toxicity to non-target organismsJ. Environ. Anal. Toxicol.S4:002(2012) 4.Amaral, T.S., Carvalho, T.F., Silva, M.C., et al.Short-term effects of a spinosyn's family insecticide on energy metabolism and liver morphology in frugivorous bats Artibeus lituratus (Olfers, 1818)Braz. J. Biol.72(2)299-304(2012) 5.Schrickx, J.A.Spinosad is a potent inhibitor of canine P-glycoproteinVet. J.200(1)195-196(2014)
| Cas No. | 168316-95-8 | SDF | |
| 别名 | LY232105, XDE-105 | ||
| Canonical SMILES | CN(C)[C@H]1CC[C@@](O[C@H]([C@@H](C)C2=O)CCC[C@H](CC)OC(C[C@]3([H])C2=C[C@]4([H])[C@@]3([H])C=C[C@@]5([H])[C@@]4([H])C[C@H](O[C@]6([H])O[C@@H](C)[C@H](OC)[C@@H](OC)[C@H]6OC)C5)=O)([H])O[C@@H]1C.CN(C)[C@H]7CC[C@@](O[C@H]([C@@H](C)C8=O)CCC[C@H](CC)OC(C[C@]9([H])C8=C[C@]%10([H])[C@@]9([H])C=C(C)[C@@]%11([H])[C@@]%10([H])C[C@H](O[C@]%12([H])O[C@@H](C)[C@H](OC)[C@@H](OC)[C@H]%12OC)C%11)=O)([H])O[C@@H]7C | ||
| 分子式 | C83H132N2O20 | 分子量 | 1478 |
| 溶解度 | Ethanol: 1 mg/ml | 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 | 0.6766 mL | 3.3829 mL | 6.7659 mL |
| 5 mM | 0.1353 mL | 0.6766 mL | 1.3532 mL |
| 10 mM | 0.0677 mL | 0.3383 mL | 0.6766 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。
Spinosad: in pediculosis capitis
Am J Clin Dermatol 2011 Oct 1;12(5):349-53.PMID:21834600DOI:10.2165/11208070-000000000-00000.
Spinosad 0.9% suspension is a topical treatment for head-lice infestation (pediculosis capitis) that has been approved in the US as a prescription medicine. Spinosad is a natural mixture of the pediculicidal tetracyclic macrolides spinosyn A and spinosyn D. Spinosad 0.9% mainly interferes with nicotinic acetylcholine receptors in insects, thereby producing neuronal excitation that results in paralysis of lice from neuromuscular fatigue after extended periods of hyperexcitation. Spinosad 0.9% kills both permethrin-susceptible and permethrin-resistant populations of lice. It is also ovicidal, killing both eggs (nits) and lice. Systemic absorption was not detectable after a single topical application of Spinosad 1.8% for 10 minutes in children. In randomized, evaluator-blind, multicenter clinical trials, topical Spinosad 0.9% without nit combing was significantly more effective than permethrin 1% with nit combing in the eradication of head lice assessed 14 days after one or two treatments. The majority of subjects treated with Spinosad 0.9% without nit combing required only a single treatment to eradicate head lice, while the majority of those treated with permethrin 1% with nit combing required two treatments. Spinosad was generally well tolerated in clinical trials, with no severe or serious adverse events. Cutaneous and ocular irritation were the most common adverse events.
Pesticide Research and Development: General Discussion and Spinosad Case
J Agric Food Chem 2022 Jul 27;70(29):8913-8919.PMID:35834192DOI:10.1021/acs.jafc.2c03821.
On average, it has taken approximately 10 years and $250 million to discover and develop one pesticide out of approximately 100 000 compounds. A successful pesticide researcher nowadays needs to be knowledgeable and skillful in multiple disciplines. As a result of the high costs and unique requirements, only a handful of companies in the world can afford to continue pesticide research and development (R/D) in the $70 billion pesticide market. Pesticide R/D is a high-risk yet high-reward business. In this perspective, pesticide R/D is briefly discussed and a case study is used to illustrate how Spinosad was discovered and became a successful product, despite the many challenges facing pesticide R/D.
Spinosad for the treatment of head lice infestations
Drugs Today (Barc) 2012 Sep;48(9):595-9.PMID:23032800DOI:10.1358/dot.2012.48.9.1844809.
Head lice infestations continue to be an issue in today's society, with an increase in economic cost and resistance. Spinosad 0.9% topical suspension was recently introduced in the U.S. market as a novel agent with both pediculicidal and ovicidal activity, approved in children 4 years of age and older for the treatment of head lice infestations. In clinical trials, it has demonstrated effectiveness against head lice with permethrin resistance. In two clinical trials comparing Spinosad to permethrin, efficacy was observed in the spinosad-treated groups at 84.6% and 86.7%, respectively, when compared to the permethrin-treated groups (respective values of 44.9% and 42.9%; P < 0.001). Overall, Spinosad was well tolerated in clinical trials.
Properties, toxicity and current applications of the biolarvicide Spinosad
J Toxicol Environ Health B Crit Rev 2020;23(1):13-26.PMID:31709913DOI:10.1080/10937404.2019.1689878.
Characterized as a highly valuable bioactive natural product, Spinosad is a pesticide with a complex chemical structure, composed of spinosyn A and D, molecules synthesized by the actinomycete Saccharopolyspora spinosa. The larvicidal activity of Spinosad was postulated to be a promising approach to combat crop pests and control species responsible to transmit mosquito-borne illness, including Aedes aegypti. Although initially deemed as relatively safe for non-target organisms and highly effective against insects and crop pests, recent studies focused on the toxicity profile detected the occurrence of side effects in different living species. Thus, the present review was undertaken to describe the properties and characteristics of Spinosad. In addition to indicating potential adverse effects on living organisms, alternative uses of the biopesticide as a mixture with different compounds are provided.
Strategies for Enhancing the Yield of the Potent Insecticide Spinosad in Actinomycetes
Biotechnol J 2019 Jan;14(1):e1700769.PMID:29897659DOI:10.1002/biot.201700769.
Spinosad is a potent insecticide that exhibits an excellent environmental and mammalian profile. However, Spinosad production in the original producer, Saccharopolyspora spinosa, is insufficient for the huge global demand. Great efforts have been exerted to improve the production of Spinosad. Strategies for Spinosad overproduction in actinomycetes are reviewed in this article, including metabolic engineering of the precursor and spinosyn biosynthetic pathway, introduction of regulatory genes, genome-scale metabolic model-guided engineering, mutagenesis, genome shuffling, fermentation process optimization, omics analysis, and the heterologous biosynthesis of Spinosad in other actinomycetes. Furthermore, highly productive industrial strains should be used as heterologous hosts for enhancing Spinosad biosynthesis in the future. To accelerate the engineering process, the CRISPR/Cas9 system should be established in Sa. spinosa for large-scale genome editing. Notably, the regulatory mechanism of Spinosad biosynthesis remains unclear. Thus, the combining multi-omics analysis with high-throughput screening of chemical elicitors would be a promising approach in characterizing the regulatory and signal transduction mechanisms and improving Spinosad production in Sa. Spinosa.