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Selamectin

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Chemical Structure| 220119-17-5 同义名 : 司拉克丁 ;UK-124114
CAS号 : 220119-17-5
货号 : A109193
分子式 : C43H63NO11
纯度 : 95%
分子量 : 769.96
MDL号 : MFCD31621085
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(136.37 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Selamectin is a semi-synthetic macrocyclic lactone that is widely used to prevent heartworm infection. Topical selamectin treatment in B. malayi and B. pahangi microfilaremic cats showed 100% effectivity in eradicating microfilaremia but only 78.5% effectivity in eliminating filarial DNA. In the chemoprophylactic group, selamectin demonstrated 66.7% efficacy in preventing B. malayi infection[3]. Fluxes of the P-gp substrate rhodamine-123 (Rh-123) across Caco-2 monolayers showed that ivermectin and selamectin acted as potent P-gp inhibitors with IC50 values of 0.1 mM[4]. A single topical application of the new spot-on formulation of selamectin plus sarolaner at the minimum label dose is effective in the treatment of adult hookworm and roundworm infections in cats[5]. The new spot-on formulation of selamectin plus sarolaner administered at monthly intervals was safe and highly effective against natural infestations of fleas and ticks on cats, and improved clinical signs of FAD (flea allergy dermatitis)[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.49mL

1.30mL

0.65mL

12.99mL

2.60mL

1.30mL
参考文献

[1]Robinson N, Brennan M. Selamectin versus ivermectin for cheyletiellosis in pet rabbits. Vet Rec. 2016 Apr 2;178(14):344-5.

[2]Hahn A, D'Agostino J, et al. Pharmacokinetics of selamectin in helmeted guineafowl (Numida meleagris) after topical administration. J Zoo Wildl Med. 2014 Mar;45(1):176-8.

[3]Sarasombath PT, Thammapalo S, Loymek S, Angkanasinsiri A, Priyavoravong P, Wongkamchai S. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019;118(4):1289‐1297

[4]Griffin J, Fletcher N, Clemence R, Blanchflower S, Brayden DJ. Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein. J Vet Pharmacol Ther. 2005;28(3):257‐265

[5]Geurden T, Vatta AF, Slootmans N, et al. Efficacy of a new spot-on formulation of selamectin plus sarolaner against Ancylostoma tubaeforme and Toxocara cati in cats. Vet Parasitol. 2017;238 Suppl 1:S31‐S35

[6]Geurden T, Becskei C, Farkas R, Lin D, Rugg D. Efficacy and safety of a new spot-on formulation of selamectin plus sarolaner in the treatment of naturally occurring flea and tick infestations in cats presented as veterinary patients in Europe. Vet Parasitol. 2017;238 Suppl 1:S12‐S17