Fluralaner
(Synonyms: 氟雷拉纳,A1443; AH252723) 目录号 : GC18295
An isoxazoline ectoparasiticide
Cas No.:864731-61-3
Sample solution is provided at 25 µL, 10mM.
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Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
Fluralaner potently inhibits flea reproduction capacity in vitro. Oviposition ceases completely at concentrations as low as 25.0 ng/mL. While no ovicidal effect is observed, fluralaner exerts a larvicidal effect at exceptionally low concentrations (6.25 ng/mL)[1].
In the simulated flea-infested home environment, flea-control efficacy on fluralaner-treated dogs is >99% at every time point measured for 12 weeks. No adverse events are observed in fluralaner-treated dogs. Fluralaner completely controls egg laying, larval development and flea reproduction even at sub-insecticidal concentrations. Oral treatment of dogs with fluralaner is highly effective for eliminating fleas in a simulated flea-infested home environment[1]. After single oral administration of Bravecto chewable tablets, mite numbers in skin scrapings are reduced by 99.8% on Day 28 and by 100% on Days 56 and 84. A marked decrease is observed in the occurrence of erythematous patches, crusts, casts and scales in the dogs treated with Bravectco[2].
References:
[1]. Williams H, et al. Fluralaner, a novel isoxazoline, prevents flea (Ctenocephalides felis) reproduction in vitro and in asimulated home environment. Parasit Vectors. 2014 Jun 19;7:275.
[2]. Walther FM, et al. Safety of fluralaner, a novel systemic antiparasitic drug, in MDR1(-/-) Collies after oral administration. Parasit Vectors. 2014 Mar 6;7:86.
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Animal experiment: |
Dogs: Thirty-two (16 male and 16 female) healthy 8-week old Beagle dogs weighing 2.0 - 3.6 kg at first administration are included in the study. Fluralaner is administered on three occasions at 8-week intervals at doses of up to 56, 168, and 280 mg fluralaner/kg body weight, equivalent to 1, 3, and 5 times the highest recommended treatment dose of fluralaner; sham dosed dogs served as controls[2]. |
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References: [1]. Williams H, et al. Fluralaner, a novel isoxazoline, prevents flea (Ctenocephalides felis) reproduction in vitro and in asimulated home environment. Parasit Vectors. 2014 Jun 19;7:275. |
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| Cas No. | 864731-61-3 | SDF | |
| 别名 | 氟雷拉纳,A1443; AH252723 | ||
| 化学名 | 4-[5-(3,5-dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-2-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-benzamide | ||
| Canonical SMILES | CC1=CC(C2=NOC(C3=CC(Cl)=CC(Cl)=C3)(C(F)(F)F)C2)=CC=C1C(NCC(NCC(F)(F)F)=O)=O | ||
| 分子式 | C22H17Cl2F6N3O3 | 分子量 | 556.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 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 | 1.7976 mL | 8.988 mL | 17.9759 mL |
| 5 mM | 0.3595 mL | 1.7976 mL | 3.5952 mL |
| 10 mM | 0.1798 mL | 0.8988 mL | 1.7976 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet