Selamectin
(Synonyms: 塞拉菌素) 目录号 : GC32174
An anthelmintic antibiotic
Cas No.:220119-17-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Animal experiment: | The cats are weighed on Days-2, 29 and 58 to calculate the dosing. Cats in group 1 (control group) remain untreated. On Day 0, the cats in group 3 are treated with fluralaner at the minimum recommending label dose of 40.0 mg per kg body weight. On Days 0, 30 and 60, the cats in group 2 are treated with the new spot-on formulation at the minimum recommending label dose of 1.0 mg/kg sarolaner and 6.0 mg/kg Selamectin. The cats are observed at different time points after treatment for possible adverse reactions to treatment. On Day 0, administration site observations are performed on all cats 30 min (±5 min), 3 h (±15 min) and 24 h (±1 h) and again on Days 3 and 5 after treatment[1]. |
References: [1]. Thomas Geurden, et al. Comparative efficacy of a new spot-on combination product containing selamectin and sarolaner (Stronghold Plus) versus fluralaner (Bravecto ) against induced infestations with Ixodes ricinus ticks on cats. Published online 2017 Jun 29. | |
Selamectin is a macrocyclic lactone derivative of ivermectin, an anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes.1,2 At 0.1 ?g/ml, selamectin is reported to inhibit growth in an H. contortus larval development assay.2
1.Holden-Dye, L., and Walker, R.J.Anthelmintic drugs and nematicides: Studies in Caenorhabditis elegansWormBook161-29(2014) 2.Michael, B., Meinke, P.T., and Shoop, W.Comparison of ivermectin, doramectin, selamectin, and eleven intermediates in a nematode larval development assayJ. Parasitol.87(3)692-696(2001)
| Cas No. | 220119-17-5 | SDF | |
| 别名 | 塞拉菌素 | ||
| Canonical SMILES | O[C@@]12[C@@]3([H])/C(C(C)=C[C@@]1([H])C(O[C@]4([H])C[C@]5(O[C@@](C/C=C(C)/[C@@H](O[C@@]6([H])C[C@@H]([C@@H](O)[C@H](C)O6)OC)[C@@H](C)/C=C/C=C2\CO3)([H])C4)O[C@H](C7CCCCC7)[C@@H](C)CC5)=O)=N\O | ||
| 分子式 | C43H63NO11 | 分子量 | 769.96 |
| 溶解度 | DMSO : 100 mg/mL (129.88 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 | 1.2988 mL | 6.4938 mL | 12.9877 mL |
| 5 mM | 0.2598 mL | 1.2988 mL | 2.5975 mL |
| 10 mM | 0.1299 mL | 0.6494 mL | 1.2988 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。
The Veterinary Anti-Parasitic Selamectin Is a Novel Inhibitor of the Mycobacterium tuberculosis DprE1 Enzyme
Int J Mol Sci 2022 Jan 11;23(2):771.PMID:35054958DOI:10.3390/ijms23020771.
Avermectins are macrocyclic lactones with anthelmintic activity. Recently, they were found to be effective against Mycobacterium tuberculosis, which accounts for one third of the worldwide deaths from antimicrobial resistance. However, their anti-mycobacterial mode of action remains to be elucidated. The activity of Selamectin was determined against a panel of M. tuberculosis mutants. Two strains carrying mutations in DprE1, the decaprenylphosphoryl-尾-D-ribose oxidase involved in the synthesis of mycobacterial arabinogalactan, were more susceptible to Selamectin. Biochemical assays against the Mycobacterium smegmatis DprE1 protein confirmed this finding, and docking studies predicted a binding site in a loop that included Leu275. Sequence alignment revealed variants in this position among mycobacterial species, with the size and hydrophobicity of the residue correlating with their MIC values; M. smegmatis DprE1 variants carrying these point mutations validated the docking predictions. However, the correlation was not confirmed when M. smegmatis mutant strains were constructed and MIC phenotypic assays performed. Likewise, metabolic labeling of selamectin-treated M. smegmatis and M. tuberculosis cells with 14C-labeled acetate did not reveal the expected lipid profile associated with DprE1 inhibition. Together, our results confirm the in vitro interactions of Selamectin and DprE1 but suggest that Selamectin could be a multi-target anti-mycobacterial compound.
Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein
J Vet Pharmacol Ther 2005 Jun;28(3):257-65.PMID:15953199DOI:10.1111/j.1365-2885.2005.00655.x.
The transport of the antiparasitic agents, ivermectin, Selamectin and moxidectin was studied in human intestinal epithelial cell monolayers (Caco-2) and canine peripheral blood lymphocytes (PBL). Both models expressed the mdr1-coded 170 kDa ATP-binding cassette (ABC) transporter P-glycoprotein (P-gp). Fluxes of the P-gp substrate rhodamine-123 (Rh-123) across Caco-2 monolayers showed that ivermectin and Selamectin acted as potent P-gp inhibitors with IC50 values of 0.1 microm. In contrast, moxidectin was a weaker P-gp inhibitor with an IC50 of 10 microm. The transport of radiolabelled ivermectin, Selamectin and moxidectin through Caco-2 monolayers showed that ivermectin, Selamectin and moxidectin were P-gp substrates with secretory/absorptive ratios of 7.5, 4.7 and 2.6 respectively. Secretory transport of [3H]-ivermectin and [3H]-selamectin was blocked by the P-gp inhibitor, verapamil. Ivermectin and Selamectin inhibited the efflux of Rh-123 from PBL and the concentration of inhibition was similar to that of verapamil. In contrast, moxidectin did not have a significant effect on Rh-123 efflux from PBL. The data suggest that ivermectin and Selamectin are potent P-gp substrates, while moxidectin is a weak one.
A review of the off-label use of Selamectin (Stronghold/Revolution) in dogs and cats
Acta Vet Scand 2008 Nov 25;50(1):46.PMID:19032763DOI:10.1186/1751-0147-50-46.
Since its introduction approximately seven years ago, Selamectin (Stronghold/Revolution, Pfizer Inc.) has been used off-label to treat a number of ecto- and endoparasite conditions in dogs and cats. It has been used as a successful prophylactic against Dirofilaria repens and as a treatment for Aelurostrongylus abstrusus in cats. It has also been used to treat notoedric mange, infestation with the nasal mite Pneumonyssoides caninum, Cheyletiella spp. and Neotrombicula autumnalis infestations and larval Cordylobia anthropophaga infection. However, to date attempts to treat generalised canine demodicosis have not been successful. In all cases, treatment was apparently well tolerated by the host.
First study of topical Selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions
Parasitol Res 2019 Apr;118(4):1289-1297.PMID:30746583DOI:10.1007/s00436-019-06248-3.
Lymphatic filariae are important human and animal parasites. Infection by these parasites could lead to severe morbidity and has significant socioeconomic impacts. Topical Selamectin is a semi-synthetic macrocyclic lactone that is widely used to prevent heartworm infection. Up until now, there were no studies that investigated the efficacy of Selamectin in lymphatic filariae. Therefore, we aimed to study the chemotherapeutic and chemoprophylactic efficacies of Selamectin use for cats in brugian filariasis-endemic areas in Southern Thailand. To assess chemotherapeutic efficacy of topical Selamectin, eight Brugia malayi and six Brugia pahangi microfilaremic cats were treated with a single administration of topical Selamectin. For chemoprophylactic efficacy assessment, a single application of topical Selamectin was administrated to 9 healthy, uninfected cats. The cats in both groups were subjected to a monthly blood testing for microfilariae and filarial DNA for 1 year. Topical Selamectin treatment in B. malayi and B. pahangi microfilaremic cats showed 100% effectivity in eradicating microfilaremia but only 78.5% effectivity in eliminating filarial DNA. In the chemoprophylactic group, Selamectin demonstrated 66.7% efficacy in preventing B. malayi infection. Our findings suggest that a single administration of 6 mg/kg topical Selamectin given every two months could effectively prevent B. malayi infection. Application of topical Selamectin twice a year could block circulating microfilariae. Since there are no treatment guidelines currently available for lymphatic filarial infection in cats, the data obtained from this study could be used to guide the management of brugian lymphatic filarial infection in reservoir cats.
Safety of Selamectin in dogs
Vet Parasitol 2000 Aug 23;91(3-4):377-91.PMID:10940536DOI:10.1016/s0304-4017(00)00306-x.
Selamectin is a broad-spectrum avermectin endectocide for treatment and control of canine parasites. The objective of these studies was to evaluate the clinical safety of Selamectin for topical use in dogs 6 weeks of age and older, including breeding animals, avermectin-sensitive Collies, and heartworm-positive animals. The margin of safety was evaluated in Beagles, which were 6 weeks old at study initiation. Reproductive, heartworm-positive, and oral safety studies were conducted in mature Beagles. Safety in Collies was evaluated in avermectin-sensitive, adult rough-coated Collies. Studies were designed to measure the safety of Selamectin at the recommended dosage range of 6-12mgkg(-1) of body weight. Endpoints included clinical examinations, clinical pathology, gross and microscopic pathology, and reproductive indices. Selected variables in the margin of safety and reproductive safety studies were subjected to statistical analyses. Pups received large doses of Selamectin at the beginning of the margin of safety study when they were 6 weeks of age and at their lowest body weight, yet displayed no clinical or pathologic evidence of toxicosis. Similarly, Selamectin had no adverse effects on reproduction in adult male and female dogs. There were no adverse effects in avermectin-sensitive Collies or in heartworm-positive dogs. Oral administration of the topical formulation caused no adverse effects. Selamectin is safe for topical use on dogs at the recommended minimum dosage of 6mgkg(-1) (6-12mgkg(-1)) monthly starting at 6 weeks of age, and including dogs of reproducing age, avermectin-sensitive Collies, and heartworm-positive dogs.