Sarolaner PF-6450567|cas:1398609-39-6|西域试剂

Sarolaner PF-6450567,99.05%

产品编号：Bellancom-16730| CAS NO：1398609-39-6| 分子式：C₂₃H₁₈Cl₂F₄N₂O₅S| 分子量：581.36

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16730	￥1500.00	杭州北京（现货）
Bellancom-16730	￥2500.00	杭州北京（现货）
Bellancom-16730	￥8500.00	杭州北京（现货）
Bellancom-16730	￥15000.00	杭州北京（现货）

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Sarolaner PF-6450567

产品介绍

Sarolaner (PF-6450567) 是具有口服活性的，广谱杀外寄生虫剂。Sarolaner 是一种异恶唑酮化合物，能有效抑制狗身上的跳蚤和虱子，对 C. felis 的 LC₈₀ 值为 0.3 μg/mL，对 O. turicata 的 LC₁₀₀ 值为 0.003 μg/mL。

生物活性

Sarolaner (PF-6450567) is an orally active and broad-spectrum ectoparasiticide. Sarolaner is an isoxazoline compound which shows efficacy against fleas and ticks on dogs, with a LC₈₀ value of 0.3 μg/mL against C. felis and a LC₁₀₀ value of 0.003 μg/mL against O. turicata.

体外研究

Sarolaner (450 nM-1 mM; 5 min) inhibits CfRDL-A285 and CfRDL-S285 receptors with γ-Aminobutyric acid (GABA)-induced currents.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	CHO-K1 cell lines
Concentration:	450 nM-1 mM
Incubation Time:	5 min
Result:	Inhibited GABA-elicited currents at both susceptible (CfRDL-A285) and resistant (CfRDL-S285) flea GABACls with EC₅₀s of 135 and 136 nM, respectively.

体内研究
(In Vivo)

Sarolaner (2.5 mg/kg; p.o. once) shows 100% efficacious against R. sanguineus and D. reticulatus.
Sarolaner (1.25- 5 mg/kg; p.o. once) effectively against I. ricinus.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Dog infested with R. sanguineus and D. reticulatus
Dosage:	2.5 mg/kg
Administration:	Oral gavage; 2.5 mg/kg once
Result:	Exibited 100% efficacy against R. sanguineus at 48 hours after treatment and also exhibited 98.0% efficacy againstD. reticulatus.

Animal Model:	Dog infested with I. ricinus
Dosage:	1.25, 2.5 and 5 mg/kg
Administration:	Oral gavage; 1.25, 2.5 and 5 mg/kg once
Result:	Exibited 100% efficacy against I. ricinus at all doses until 7 days, and provided over 99.3% reduction against subsequent re-infestations until 57 days at dose of 5.0 and 2.5 mg/kg.

体内研究

Sarolaner (2.5 mg/kg; p.o. once) shows 100% efficacious against R. sanguineus and D. reticulatus.
Sarolaner (1.25- 5 mg/kg; p.o. once) effectively against I. ricinus.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Dog infested with R. sanguineus and D. reticulatus
Dosage:	2.5 mg/kg
Administration:	Oral gavage; 2.5 mg/kg once
Result:	Exibited 100% efficacy against R. sanguineus at 48 hours after treatment and also exhibited 98.0% efficacy againstD. reticulatus.

Animal Model:	Dog infested with I. ricinus
Dosage:	1.25, 2.5 and 5 mg/kg
Administration:	Oral gavage; 1.25, 2.5 and 5 mg/kg once
Result:	Exibited 100% efficacy against I. ricinus at all doses until 7 days, and provided over 99.3% reduction against subsequent re-infestations until 57 days at dose of 5.0 and 2.5 mg/kg.

体内研究

Sarolaner (2.5 mg/kg; p.o. once) shows 100% efficacious against R. sanguineus and D. reticulatus.
Sarolaner (1.25- 5 mg/kg; p.o. once) effectively against I. ricinus.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Dog infested with R. sanguineus and D. reticulatus
Dosage:	2.5 mg/kg
Administration:	Oral gavage; 2.5 mg/kg once
Result:	Exibited 100% efficacy against R. sanguineus at 48 hours after treatment and also exhibited 98.0% efficacy againstD. reticulatus.

Animal Model:	Dog infested with I. ricinus
Dosage:	1.25, 2.5 and 5 mg/kg
Administration:	Oral gavage; 1.25, 2.5 and 5 mg/kg once
Result:	Exibited 100% efficacy against I. ricinus at all doses until 7 days, and provided over 99.3% reduction against subsequent re-infestations until 57 days at dose of 5.0 and 2.5 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 300 mg/mL (516.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7201 mL	8.6005 mL	17.2010 mL
5 mM	0.3440 mL	1.7201 mL	3.4402 mL
10 mM	0.1720 mL	0.8601 mL	1.7201 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 7.5 mg/mL (12.90 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (12.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 7.5 mg/mL (12.90 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (12.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。