Sarolaner   中文名称: 沙罗拉纳

Sarolaner（450 nM-1 mM；5 分钟）抑制 CfRDL-A285 和 CfRDL-S285 受体上伽马缓冲丁酸 (GABA) 产生的电流 [1]。

Sarolaner 在 2.5 mg/kg 剂量下对 R 表现出 100% 的有效性；主侧壁。 sanguineus 以及 D. reticuLatus [1]。 Sarolaner 作用于 I，在 1.25-5 mg/kg（初级侧壁）时有效。蓖麻[1]。

细胞活力测定[1]
细胞类型： CHO-K1 细胞
测试浓度： 450 nM-1 mM
孵育时间： 5分钟
实验结果：对敏感跳蚤(CfRDL-A285)和抗性跳蚤GABAC1引起的GABA电流的抑制，EC50分别为135和136 nM。

Animal/Disease Models: Dogs infected with R. sanguineus and D. reticulatus [1]
Doses: 2.5 mg/kg
Route of Administration: po (oral gavage); 2.5 mg/kg One time
Experimental Results:100% efficacy against R. sanguineus 48 hrs (hrs (hours)) after treatment , also has 98.0% efficacy against D. d. Net pattern.

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Animal/Disease Models: Ricin-infected dogs [1] Doses: 1.25, 2.5 and 5 mg/kg
Route of Administration: po (oral gavage); 1.25, 2.5 and 5 mg/kg Primary
Experimental Results: Prior to 7 days, all doses were effective in ricin Both narcotics demonstrated 100% efficacy and diminished subsequent reinfections by more than 99.3% by 57 days at doses of 5.0 and 2.5 mg/kg.

[1]. Discovery of sarolaner: A novel, orally administered, broad-spectrum, isoxazoline ectoparasiticide for dogs. Vet Parasitol. 2016 May 30;222:3-11.

See also: Moxidectin; Pyrantel Pamoate; Sarolaner (component of); Sarolaner; Selamectin (component of).

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Drug Indication
For the treatment of tick infestations (Dermacentor reticulatus, Ixodes hexagonus, Ixodes ricinus and Rhipicephalus sanguineus). The veterinary medicinal product has immediate and persistent tick killing activity for at least 5 weeks. For the treatment of flea infestations (Ctenocephalides felis and Ctenocephalides canis). The veterinary medicinal product has immediate and persistent flea killing activity against new infestations for at least 5 weeks. The veterinary medicinal product can be used as part of a treatment strategy for the control of Flea Allergy Dermatitis (FAD). For the treatment of sarcoptic mange (Sarcoptes scabiei). For the treatment of ear mite infestations (Otodectes cynotis). For the treatment of demodicosis (Demodex canis). Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance.
For the treatment of tick infestations (Dermacentor reticulatus, Ixodes hexagonus,Ixodes ricinus and Rhipicephalus sanguineus). The veterinary medicinal product has immediate and persistent tick killing activity for at least 5 weeks. , , For the treatment of flea infestations (Ctenocephalides felis and Ctenocephalides canis). The veterinary medicinal product has immediate and persistent flea killing activity against new infestations for at least 5 weeks. The veterinary medicinal product can be used as part of a treatment strategy for the control of Flea Allergy Dermatitis (FAD). , , For the treatment of sarcoptic mange (Sarcoptes scabiei). , , For the treatment of ear mite infestations (Otodectes cynotis). , , For the treatment of demodicosis (Demodex canis). , , Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance. ,

C23H18CL2F4N2O5S

581.364037036896

580.025

1398609-39-6

73169092

White to off-white solid powder

4.781

93.65

0

10

4

37

1050

1

CS(=O)(=O)CC(=O)N1CC2(C1)C3=C(CO2)C=C(C=C3)C4=NO[C@@](C4)(C5=CC(=C(C(=C5)Cl)F)Cl)C(F)(F)F

FLEFKKUZMDEUIP-QFIPXVFZSA-N

InChI=1S/C23H18Cl2F4N2O5S/c1-37(33,34)9-19(32)31-10-21(11-31)15-3-2-12(4-13(15)8-35-21)18-7-22(36-30-18,23(27,28)29)14-5-16(24)20(26)17(25)6-14/h2-6H,7-11H2,1H3/t22-/m0/s1

(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

PF6450567; PF 6450567; PF-6450567

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~300 mg/mL (~516.03 mM)

配方 1 中的溶解度: ≥ 7.5 mg/mL (12.90 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 75.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 7.5 mg/mL (12.90 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 75.0 mg/mL 澄清 DMSO 储备液加入900 μL 玉米油中，混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。