Eprinomectin B1a
(Synonyms: 依立诺克丁B1A) 目录号 : GC40845
A major component of eprinomectin
Cas No.:133305-88-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eprinomectin B1a is a major component (>90%) of the antiparasitic compound eprinomectin, which also contains eprinomectin B1b and belongs to the avermectin family of insecticides and anthelmintics.
| Cas No. | 133305-88-1 | SDF | |
| 别名 | 依立诺克丁B1A | ||
| Canonical SMILES | C/C([C@@H](O[C@@]1([H])C[C@H](OC)[C@@H](O[C@]2([H])O[C@@H](C)[C@@H](NC(C)=O)[C@@H](OC)C2)[C@H](C)O1)[C@@H](C)/C=C/C=C(CO3)/[C@@]([C@@]3([H])[C@H](O)C(C)=C4)(O)[C@]4([H])C5=O)=C\C[C@]6([H])C[C@@](O5)([H])C[C@]7(C=C[C@H](C)[C@]([C@H](CC)C)([H])O7)O6 | ||
| 分子式 | C50H75NO14 | 分子量 | 914.1 |
| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.094 mL | 5.4699 mL | 10.9397 mL |
| 5 mM | 0.2188 mL | 1.094 mL | 2.1879 mL |
| 10 mM | 0.1094 mL | 0.547 mL | 1.094 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。
Pharmacokinetics and metabolism of eprinomectin in cats when administered in a novel topical combination of fipronil, (S)-methoprene, eprinomectin and praziquantel
Vet Parasitol 2014 Apr 28;202(1-2):2-9.PMID:24703069DOI:10.1016/j.vetpar.2014.02.031.
Four studies were conducted to determine the pharmacokinetic characteristics and in vitro metabolism of eprinomectin, a semi-synthetic avermectin, in cats. Pharmacokinetic parameters including bioavailability of eprinomectin were determined in a parallel study design comprised of one group of eight cats which were treated once topically at 0.12 mL/kg bodyweight with BROADLINE(®), a novel combination product (fipronil 8.3% (w/v), (S)-methoprene 10% (w/v), eprinomectin 0.4% (w/v) and praziquantel 8.3% (w/v)), delivering a dose of 0.5mg eprinomectin per kg body weight, and a group of six cats which received 0.4% (w/v) eprinomectin at 0.4 mg/kg bodyweight once by intravenous injection. For cats treated by topical application, the average eprinomectin (B1a component) maximum plasma concentration (Cmax) was 20 ng/mL. The maximum concentrations were reached 24h after dosing in the majority of the animals (six of eight cats). The average terminal half-life was 114 h due to slow absorption ('flip-flop' kinetics). Following intravenous administration the average Cmax was 503 ng/mL at 5 min post-dose, and the mean elimination half-life was 23 h. Eprinomectin was widely distributed with a mean volume of distribution of 2,390 mL/kg, and the clearance rate was 81 mL/h/kg. Mean areas under the plasma concentration versus time curves extrapolated to infinity were 2,100 ngh/mL and 5,160 ngh/mL for the topical and intravenous doses, respectively. Topical eprinomectin was absorbed with an average absolute bioavailability of 31%. In a second parallel design study, the dose proportionality of eprinomectin after single topical administration of BROADLINE(®) was studied. Four groups of eight cats each were treated once topically with 0.5, 1, 2 or 5 times the minimum recommended dose of the combination, 0.12 mL/kg bodyweight. Based on comparison of areas under the plasma concentration versus time curves from the time of dosing to the last time point at which Eprinomectin B1a was quantified, and Cmax, dose proportionality was established. In addition, the metabolic pathway of eprinomectin using cat liver microsomes, and plasma protein binding using cat, rat, and dog plasma were studied in vitro. Results of the analyses of Eprinomectin B1a described here showed that it is metabolically stable and highly protein bound (>99%), and thus likely to be, as with other species, excreted mainly as unchanged parent drug in the feces of cats.
The environmental safety of eprinomectin to earthworms
Vet Parasitol 2005 Mar 10;128(1-2):109-14.PMID:15725539DOI:10.1016/j.vetpar.2004.11.007.
A study was conducted to assess the environmental safety of the endectocide eprinomectin to the earthworm Lumbricus terrestris under conditions mimicking typical product use on pasture. The LC50 value of eprinomectin in artificial soil after 28 days of exposure is higher than the levels expected in feces from dosed cattle or in soil fertilized with manure from dosed cattle, which indicates a wide margin of safety for this compound to earthworms. However, the no-observed-effect concentration has not been established. Therefore, the current study was conducted to determine whether there would be any effects on earthworms from feces from cattle treated with the commercial formulation of eprinomectin. Feces were collected rectally from grazing cattle on Day 0 before treatment and on Days 2, 4, 7 and 14 after treatment with EPRINEX (eprinomectin) Pour-On for Beef and Dairy Cattle (Merial Limited) at 0.5 mg eprinomectin per kg bodyweight. Assays of Eprinomectin B1a (the major component of eprinomectin) were 0, 0.427, 0.152, 0.0512 and 0.00185 mg kg-1 wet weight of feces (equivalent to 0, 3.34, 1.19, 0.40 and 0.010 mg kg-1 on a dry weight basis, respectively). No significant differences (p>0.05) were observed at any day post-treatment in the survival or behavioral effects of any worms fed post-dose feces relative to the worms fed control feces. All post-dose comparisons of weight changes of living earthworms to the control group were not significantly different (p>0.05), indicating that treatment of cattle with EPRINEX (eprinomectin) Pour-On for Beef and Dairy Cattle did not affect feeding or weight gain of the earthworms. The LC50 value and the results of this study establish the wide margin of safety afforded to earthworms by eprinomectin under typical usage conditions.
Reevaluation of efficacy against nematode parasites and pharmacokinetics of topical eprinomectin in cattle
Parasitol Res 2012 Sep;111(3):1343-7.PMID:22638921DOI:10.1007/s00436-012-2970-2.
A study was conducted to confirm the efficacy of topical eprinomectin against nematodes and to evaluate the pharmacokinetics in cattle prevented from having physical contact with other cattle and from self-grooming. Sixteen male Brown Swiss calves were infected with larvae of recently isolated nematode parasites. Inoculation was scheduled so that the nematodes were expected to be adults at the time of treatment. Animals were blocked based on pretreatment body weight and randomly allocated to the untreated control group or the group treated with EPRINEX® Pour-On (Merial; 0.5 mg eprinomectin per kilogram body weight). Plasma samples were collected prior to and between 1 and 21 days following treatment and analysed for eprinomectin (B1a component) concentrations. For parasite recovery, identification and counting, animals were humanely euthanized 21 days after treatment. Calves treated with eprinomectin had significantly (p < 0.05) fewer (>99 % reduction) adult Dictyocaulus viviparus, Bunostomum phlebotomum, Cooperia oncophora, Cooperia surnabada, Cooperia punctata, Nematodirus helvetianus, Oesophagostomum radiatum, Ostertagia ostertagi, Ostertagia lyrata, and Trichostrongylus axei and inhibited fourth-stage Nematodirus and Ostertagia larvae than the controls. The main pharmacokinetic parameters of Eprinomectin B1a were: AUC(inf), 124 ± 24 day ng/mL; T (1/2), 5.2 ± 0.9 days; and C (max), 9.7 ± 2.2 ng/mL. Individual maximal concentrations were observed 3-7 days after treatment. This study confirmed the continued high level of efficacy of topically administered eprinomectin against a wide range of recently isolated nematodes. In addition, this study demonstrates that oral ingestion is not required to achieve adequate exposure for efficacy following topical administration of eprinomectin.
Pharmacokinetics and anthelmintic efficacy of topical eprinomectin in goats prevented from grooming
Parasitol Res 2014 Nov;113(11):4039-44.PMID:25106840DOI:10.1007/s00436-014-4072-9.
Pharmacokinetics and anthelmintic activity of topical eprinomectin in goats prevented from physical contact to others and self-grooming were studied. Sixteen approximately 7 months old male castrated German White Noble goats harbouring induced infections of gastrointestinal nematode parasites were included in the study. They were blocked based on pre-treatment body weight (range 22.4 to 36.4 kg) and then randomly allocated to the untreated control group or the group treated with topical 0.5% w/v eprinomectin (EPRINEX Pour-on, Merial) at 1 mg/kg body weight. Plasma samples were collected prior to and at intervals up to 14 days following treatment and analyzed to determine the concentrations of eprinomectin (B1a component). Parasites were recovered, identified, and counted following necropsy 14 days after treatment. Goats treated with topical eprinomectin had significantly fewer (≥99% reduction, p < 0.01) adult Cooperia curticei, Haemonchus contortus, Nematodirus battus, Oesophagostomum venulosum, Ostertagia circumcincta, and Trichostrongylus colubriformis than the untreated controls. Basic pharmacokinetic parameters for Eprinomectin B1a were AUCinfinity, 37.1 ± 15.2 day ng/mL; T½, 5.11 ± 2.83 days; and Cmax, 5.93 ± 1.87 ng/mL; individual maximal concentrations were observed 1 or 2 days after treatment. Results of this study indicate that oral ingestion is not required to achieve adequate exposure for excellent anthelmintic efficacy following topical administration of eprinomectin at 1 mg/kg body weight to goats.
Simultaneous determination of avermectins in bovine tissues by LC-MS/MS
J Sep Sci 2009 Nov;32(21):3596-602.PMID:19877150DOI:10.1002/jssc.200900411.
Analytical method for the simultaneous quantification of avermectins (AVMs), abamectin B1a, abamectin 8,9-Z isomer B1a, emamectine benzoate B1a, emamectine benzoate 8,9-Z isomer B1a, ivermectin, Eprinomectin B1a, doramectin and moxidectin in bovine tissues (muscle, liver and fat) was developed by LC-MS/MS in electrospray positive ion mode. The separation was achieved on a short TSK-GEL ODS 100V column with the mobile phase consisting of acetonitrile and aquatic 0.1 mM ammonium formate containing 0.1% formic acid v/v at a flow rate of 0.2 mL/min with gradient elution. Liquid-liquid extraction with isooctane was used for the sample extraction/preparation of analytes in bovine samples. The linearity of the calibration curves was excellent in matrix-matched standards, and yielded the coefficients (r(2)=0.997-0.999, range from LOQ to 500, 1000 or 5000 ng/g) of determination of the target analytes. Recoveries were in the range of 87.9-99.8% with associated precision values (within-day: 1.5-7.4%, n=6, and between-day: 1.5-8.4% for 3 days) for repeatability and reproducibility. LC-MS/MS method has been proven to be highly efficient and suitable for the simultaneous determinations of eight AVMs in bovine tissue samples.