(S)-(+)-Methoprene
(Synonyms: S-(+)-烯虫酯,(+)-Methoprene; (7S)-Methoprene) 目录号 : GC46347
An insect growth regulator and Met agonist
Cas No.:65733-16-6
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
(S)-(+)-Methoprene is a widely-used insect growth regulator.1 It is remarkable for its lack of significant effects against a wide variety of mammals, although concerns remain for its effects on arthropod development.1,2 Methoprene acts as an activator of the juvenile hormone receptor, known as Methoprene-tolerant or Met (Kd = 12.3 nM).3,4 Met is a transcription factor that, upon activation with juvenile hormone or methoprene, regulates gene expression that inhibits metamorphosis.5
1.Siddall, J.B.Insect growth regulators and insect control: A critical appraisalEnvironmental Health Perspectives14119-126(1976) 2.Wright, J.E.Environmental and toxicological aspects of insect growth regulatorsEnvironmental Health Perspectives14127-132(1976) 3.Charles, J.P., Iwema, T., Epa, V.C., et al.Ligand-binding properties of a juvenile hormone receptor, methoprene-tolerantProceedings of the National Academy of Sciences of the United States of America108(52)21128-21133(2011) 4.Osir, E.O., and Riddiford, L.M.Nuclear binding sites for juvenile hormone and its analogs in the epidermis of the tobacco hornwormThe Journal of Biological Chemisty263(27)13812-13818(1988) 5.Zou, Z., Saha, T.T., Roy, S., et al.Juvenile hormone and its receptor, methoprene-tolerant, control the dynamics of mosquito gene expressionProceedings of the National Academy of Sciences of the United States of America110(24)E2173-E2181(2013)
| Cas No. | 65733-16-6 | SDF | |
| 别名 | S-(+)-烯虫酯,(+)-Methoprene; (7S)-Methoprene | ||
| Canonical SMILES | CC(C)OC(/C=C(C)/C=C/C[C@@H](C)CCCC(OC)(C)C)=O | ||
| 分子式 | C19H34O3 | 分子量 | 310.5 |
| 溶解度 | DMF: 20 mg/ml,Ethanol: 10 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 | 3.2206 mL | 16.1031 mL | 32.2061 mL |
| 5 mM | 0.6441 mL | 3.2206 mL | 6.4412 mL |
| 10 mM | 0.3221 mL | 1.6103 mL | 3.2206 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 fipronil/(S)-methoprene/eprinomectin/praziquantel (Broadline®) against Thelazia callipaeda in naturally infected cats
Parasit Vectors 2021 Sep 15;14(1):477.PMID:34526129DOI:10.1186/s13071-021-04983-0.
Background: The present clinical field trial was conducted to assess the efficacy of a broad-spectrum parasiticide spot-on formulation containing eprinomectin (Broadline®) against Thelazia callipaeda eyeworm in naturally infected cats. Methods: Fifteen privately owned cats harboring at least one live adult T. callipaeda were included in the study. Cats were randomly allocated to an untreated control group of seven cats or to a Broadline®-treated group of eight cats. Cats were treated on Day 0; ocular examinations were performed at inclusion and on Days 7 and 14; eyeworms were recovered and counted on Day 14. The primary efficacy assessment was based on group comparison of number of T. callipaeda on Day 14. Results: Seven days after treatment, six of eight treated cats were negative for eyeworm infection per visual examination, and on Day 14 no eyeworms were found in the treated cats while the seven untreated cats were still infected (geometric mean: 1.97). All cats had inflammatory ocular signs at inclusion; on Day 14, five of eight treated cats had recovered while all untreated control cats were still symptomatic. All collected parasites were confirmed to be T. callipaeda by morphology and molecular characterization. Conclusions: A single treatment with Broadline® provided 100% efficacy against feline thelaziosis and improved related ocular inflammation signs.
Efficacy of two endectoparasiticide products combining fipronil and (S)-methoprene or esafoxolaner with eprinomectin and praziquantel against fleas and intestinal helminths in cats naturally infested in Brazil
Parasite 2022;29:12.PMID:35238771DOI:10.1051/parasite/2022012.
Eprinomectin and praziquantel, nematodicide and cestodicide compounds, are both combined with the insecticide and acaricide compounds fipronil and (S)-methoprene in Frontline® Protect/Broadline®, or esafoxolaner in NexGard® Combo. These topical feline endectoparasiticide products were tested for efficacy against fleas and intestinal helminths in a field trial in Brazil. Flea- and/or helminth-infested domestic cats were treated twice at a monthly interval following label instructions: 160 cats with Frontline® Protect/Broadline® and 165 cats with NexGard® Combo. The flea and intestinal helminth infestations were evaluated using comb counts and copromicroscopy, respectively before first treatment for baseline value, then 9 and 30 days after each treatment for fleas, and 9 days after each treatment for helminths. Multiparasitism was very frequent at baseline, as amongst the 325 included cats, 295, 280, 86 and 93 cats were at least infested with Ctenocephalides fleas, Ancylostoma, Toxocara and Dipylidium caninum, respectively. Efficacies were calculated by comparing the geometric means at baseline and at post-treatment timepoints for each parasite genus/species. Inclusive of both products and of all evaluation timepoints, the Ctenocephalides, Ancylostoma, Toxocara and D. caninum efficacies were at least 98.3%, 99.8%, 99.8% and 96.3%, respectively. No adverse reactions were observed, except for a few instances of mild, transient, and self-resolving hypersalivation occurring on the day of treatment in both groups. This field trial demonstrated high-level efficacy of Frontline® Protect/Broadline® and NexGard® Combo against major parasites of cats in Brazil.
Evaluation of indoxacarb and fipronil (S)-methoprene topical spot-on formulations to control flea populations in naturally infested dogs and cats in private residences in Tampa FL. USA
Parasit Vectors 2013 Dec 28;6:366.PMID:24373508DOI:10.1186/1756-3305-6-366.
Background: A study was conducted to evaluate and compare the effectiveness of two different spot-on topical flea products to control flea infestations on naturally infested dogs and cats in Tampa, FL USA. Methods: Thirty-two dogs and 3 cats with natural flea infestations living in 18 homes were treated topically with a 19.53% w/w spot-on formulation of indoxacarb. Another thirty dogs and 2 cats living in 19 different homes were treated topically with either fipronil (9.8% w/w)/(S)-methoprene (8.89% w/w) or fipronil (9.8% w/w)/(S)-methoprene (11.8% w/w), respectively. All products were applied according to label directions by study investigators on day 0 and again between days 28 and 30. Flea populations on pets were assessed using visual area counts and premise flea infestations were assessed using intermittent-light flea traps on days 0, 7, 14, 21, 28-30, 40-45, and 54-60. Results: A single application of the indoxacarb or fipronil (S)-methoprene formulations reduced flea populations on pets by 97.8% and 85.5%, respectively within 7 days. One month (28-30 days) after treatment the indoxacarb and fipronil (S)-methoprene formulations reduced on-animal flea burdens by 95.0% and 49.5%, respectively. Following two monthly applications of either the indoxacarb or fipronil (S)-methoprene formulations, pet flea burdens were reduced by 99.1% and 54.8%, respectively, by days 54-60. At the end of the two month study, 77.1% and 15.6% of the dogs and cats in the indoxacarb and fipronil (S)-methoprene treatment groups, respectively were flea free. Flea numbers in the indoor-premises were markedly reduced in both treatment groups by days 54-60, with 97.7% and 84.6% reductions in intermittent-light flea trap counts in the indoxacarb and fipronil (S)-methoprene treatment groups, respectively. Conclusions: This in-home investigation conducted during the summer of 2013 in subtropical Tampa, FL, is the first published U.S field investigation of the indoxacarb topical formulation. The indoxacarb formulation was able to effectively control flea populations in heavily flea infested pets and homes. The efficacy achieved by the fipronil (S)-methoprene formulation against flea infestations on these pets was lower than in previous investigations using the same study design.
The actions of benzophenanthridine alkaloids, piperonyl butoxide and (S)-methoprene at the G-protein coupled cannabinoid CB₁ receptor in vitro
Eur J Pharmacol 2011 Mar 1;654(1):26-32.PMID:21172340DOI:10.1016/j.ejphar.2010.11.033.
This investigation focused primarily on the interaction of two benzophenanthridine alkaloids (chelerythrine and sanguinarine), piperonyl butoxide and (S)-methoprene with G-protein-coupled cannabinoid CB(1) receptors of mouse brain in vitro. Chelerythrine and sanguinarine inhibited the binding of the CB(1) receptor agonist [(3)H]CP-55940 to mouse whole brain membranes at low micromolar concentrations (IC(50)S: chelerythrine 2.20 μM; sanguinarine 1.10 μM). The structurally related isoquinoline alkaloids (berberine and papaverine) and the phthalide isoquinoline ((-)-β-hydrastine) were either inactive or considerably below IC(50) at 30 μM. Chelerythrine and sanguinarine antagonized CP-55940-stimulated binding of [(35)S] GTPγS to the G-protein (IC(50)S: chelerythrine 2.09 μM; sanguinarine 1.22 μM). In contrast to AM251, both compounds strongly inhibited basal binding of [(35)S]GTPγS (IC(50)S: chelerythrine 10.06 μM; sanguinarine 5.19μM). Piperonyl butoxide and S-methoprene inhibited the binding of [(3)H]CP-55940 (IC(50)S: piperonyl butoxide 8.2 μM; methoprene 16.4 μM), and also inhibited agonist-stimulated (but not basal) binding of [(35)S]GTPγS to brain membranes (IC(50)S: piperonyl butoxide 22.5 μM; (S)-methoprene 19.31 μM). PMSF did not modify the inhibitory effect of (S)-methoprene on [(3)H]CP-55940 binding. Our data suggest that chelerythrine and sanguinarine are efficacious antagonists of G-protein-coupled CB(1) receptors. They exhibit lower potencies compared to many conventional CB(1) receptor blockers but act differently to AM251. Reverse modulation of CB(1) receptor agonist binding resulting from benzophenanthridines engaging with the G-protein component may explain this difference. Piperonyl butoxide and (S)-methoprene are efficacious, low potency, neutral antagonists of CB(1) receptors. Certain of the study compounds may represent useful starting structures for development of novel/more potent G-protein-coupled CB(1) receptor blocking drugs.
Evaluation and comparison of a flumethrin-imidacloprid collar and repeated monthly treatments of fipronil/(S)-methoprene to control flea, Ctenocephalides f. felis, infestations on cats for eight months
Parasit Vectors 2016 May 17;9(1):287.PMID:27189592DOI:10.1186/s13071-016-1575-5.
Background: This controlled laboratory study was designed to evaluate the efficacy of the 10 % imidacloprid/4.5 % flumethrin collar (Seresto®, Bayer Animal Health) against fleas (Ctenocephalides f. felis) on cats, when compared to fipronil (9.8 %w/w)/(S)-methoprene (11.8 % w/w) topical spot-on formulation (Frontline® Plus for Cats and Kittens, Merial). Methods: Thirty cats were randomized into three groups of ten animals based on pre-treatment flea counts: Group 1: imidacloprid/flumethrin collar; Group 2: fipronil/(S)-methoprene topical spot-on and Group 3: non-treated controls. The imidacloprid/flumethrin collars were applied one time on Day 0, while the fipronil/(S)-methoprene spot-on was administered every 30 days from Day 0 through Day 210. Cats were infested with 100 fleas on study days 0, 7, 14, 29, 59, 89, 119, 149, 179, 209 and 239. All flea counts were conducted by combing to remove fleas on post-treatment days 2, 8, 15, 30, 60, 90, 120, 150, 180, 210 and 240. Results: The efficacy of the imidacloprid/flumethrin collar ranged from 98.2 to 100 % for eight months. The efficacy of fipronil/(S)-methoprene spot-on ranged from 68.2 to 99.9 %. Efficacy was < 85 % for fipronil/(S)-methoprene on Days 90, 150 and 210. The flea counts in both treatment groups were significantly fewer than those in the non-treated control group at every post-treatment study day (P < 0.0001). In addition, there were significantly fewer fleas in the imidacloprid/flumethrin collar group when compared to the fipronil/(S)-methoprene group on Days 90, 150 and 210 (P < 0.0001). Conclusions: This study demonstrated that the imidacloprid/flumethrin collar (Seresto®, Bayer Animal Health) maintained excellent ( > 98.2 %) efficacy against fleas on cats for the entire 8 month study. Monthly applications of fipronil/(S)-methoprene (Frontline® Plus for Cats and Kittens, Merial) generally had high, but variable (68.2 to 99.9 %) efficacy over the course of the eight month study. Based on the very high residual efficacy achieved by the imidacloprid/flumethrin collar in this study, veterinarians should expect that this collar will control and eliminate existing flea infestations on cats and in their in-home premises as long as every flea infested host is treated.