Sarolaner
(Synonyms: 1-[5'-[(5S)-5-(3,5-二氯-4-氟苯基)-4,5-二氢-5-(三氟甲基)-3-异恶唑基]螺[氮杂环丁烷-3,1'(3'H)-异苯并呋喃]-1-基]-2-(甲基磺酰基)乙酮,PF-6450567) 目录号 : GC34774
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Sarolaner是一种口服的、广谱的异噁唑啉类犬体外寄生虫杀灭剂。
Cas No.:1398609-39-6
Sample solution is provided at 25 µL, 10mM.
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Sarolaner is an orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs [1].
In vitro sarolaner demonstrated an LC80 of 0.3μg/mL against C. felis and an LC100 of 0.003μg/mL against O. turicata [1].
In vivo efficacy (> 99%) of sarolaner was demonstrated against fleas and ticks for at least one month from a single oral dose of between 1.25 and 5mg/kg in dogs [1]. Sarolaner at an oral dose of 2mg/kg was highly effective in reducing the live mite counts in dogs with a natural infestation of Demodex spp. and an induced infestation of O. cynotis [2]. Oral administration of sarolaner at 2–4mg/kg achieved >95% efficacy against the feline fur mite Lynxacarus radovskyi at Day 30 post-treatment [3].
References:
[1] McTier, Tom L., et al. "Discovery of sarolaner: A novel, orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs." Veterinary Parasitology 222 (2016): 3-11.
[2] Six, Robert H., et al. "Efficacy of sarolaner, a novel oral isoxazoline, against two common mite infestations in dogs: Demodex spp. and Otodectes cynotis." Veterinary Parasitology 222 (2016): 62-66.
[3] Campos, Diefrey R., et al. "Efficacy of oral sarolaner against Lynxacarus radovskyi in naturally infested cats." Veterinary Dermatology 31.5 (2020): 355-e92.
Sarolaner是一种口服的、广谱的异噁唑啉类犬体外寄生虫杀灭剂 [1]。
体外实验中，Sarolaner对跳蚤（Ctenocephalides felis）的LC80为 0.3μg/mL，对软蜱(Ornithodoros turicata)的LC100为 0.003μg/mL [1]。
体内试验中，Sarolaner （1.25 and 5mg/kg）给狗口服，对跳蚤和蜱虫的杀灭效果(> 99%)至少能持续一个月[1]。口服剂量为 2mg/kg 的Sarolaner能有效降低自然感染Demodex spp.和人为感染O. cynotis的犬体内活螨的数量 [2]。给猫单次口服Sarolaner 2-4mg/kg，治疗后 30 天对猫毛螨 Lynxacarus radovskyi 的清除效果达到 95% 以上 [3]。
| Animal experiment [1]: | |
Animal models | Beagles dogs |
Preparation Method | On Day-7, each dog was infested with Rhipicephalus sanguineus. On Day-5, the ticks on each dog were counted, dogs were ranked by descending tick count into blocks, and randomly allocated within blocks to two treatment groups of eight dogs each. On Day-2, the dogs were weighed and infested with R. sanguineus and Dermacentor reticulatus ticks. On Day-1, the dogs were infested with fleas. On Day 0, each animal was treated via oral gavage at 0.5mL/kg body weight with either placebo control or sarolaner solution (5mg/mL) to provide a dose of 2.5mg/kg. A tetraglycol/solutol solution base was used to formulate the sarolaner. Dogs were observed for general health and any reaction to treatment approximately 1, 3 and 6h after treatment on Day 0, then once daily for the remainder of the study. On Day 2, each dog was examined and combed to count and remove fleas and ticks. Subsequently, all animals were infested with R. sanguineus and D. reticulatus on Days 5, 12, 19, 25 and 33, and with fleas on Days 6, 13, 20, 26 and 34. All dogs were examined, combed and parasite counted on Days 7, 14, 21, 27 and 35. |
Dosage form | 2.5mg/kg; oral gavage; once |
Applications | Sarolaner was 100% efficacious at 48h after treatment and against subsequent infestations through Day 35. |
References: | |
| Cas No. | 1398609-39-6 | SDF | |
| 别名 | 1-[5'-[(5S)-5-(3,5-二氯-4-氟苯基)-4,5-二氢-5-(三氟甲基)-3-异恶唑基]螺[氮杂环丁烷-3,1'(3'H)-异苯并呋喃]-1-基]-2-(甲基磺酰基)乙酮,PF-6450567 | ||
| Canonical SMILES | O=S(CC(N1CC2(OCC3=C2C=CC(C4=NO[C@](C(F)(F)F)(C5=CC(Cl)=C(F)C(Cl)=C5)C4)=C3)C1)=O)(C)=O | ||
| 分子式 | C23H18Cl2F4N2O5S | 分子量 | 581.36 |
| 溶解度 | DMSO : 150 mg/mL (258.02 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at 4°C, sealed storage, away from moisture |
| 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 | 1.7201 mL | 8.6005 mL | 17.201 mL |
| 5 mM | 344 μL | 1.7201 mL | 3.4402 mL |
| 10 mM | 172 μL | 860.1 μL | 1.7201 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
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet