Sarolaner
目录号: PL08867 纯度: ≥99%
CAS No. :1398609-39-6
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中文名称
Sarolaner
中文别名
1-[6-[(5S)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]spiro[1H-2-benzofuran-3,3'-azetidine]-1'-yl]-2-methylsulfonylethanone;沙罗拉纳
英文名称
Sarolaner
英文别名
Sarolaner;DM113FTW7F;1-[6-[(5S)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]spiro[1H-2-benzofuran-3,3'-azetidine]-1'-yl]-2-methylsulfonylethanone;(S)-1-(5'-(5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'H-spiro[azetidine-3,1'-isobenzofuran]-1-yl)-2-(methylsulfonyl)ethan-1-one;Sarolaner [USAN:INN];Simparica;Sarolaner (USAN/INN);1-(5'-((5S)-5-(3,5;PF-6450567
Cas No.
1398609-39-6
分子式
C23H18Cl2F4N2O5S
分子量
581.36
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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 LC 80 value of 0.3 μg/mL against C. felis and a LC 100 value of 0.003 μg/mL against O. turicata.
性状
Solid
IC50 & Target[1][2]
LC80: 0.3μg/mL (C. felis)
LC100: 0.003 μg/mL (O. turicata)
IC50: 135 nM (CfRDL-A285), 136 nM (CfRDL-S285)
体外研究(In Vitro)
Sarolaner (450 nM-1 mM; 5 min) inhibits CfRDL-A285 and CfRDL-S285 receptors with γ-Aminobutyric acid (GABA)-induced currents. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. McTier TL, et al. Discovery of sarolaner: A novel, orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs. Vet Parasitol. 2016 May 30;222:3-11.
溶解度数据
In Vitro: DMSO : 300 mg/mL (516.03 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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