SelamectinSelamectin
MedChemExpress (MCE)
HY-107212
220119-17-5
99.05%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
The transport of radiolabelled Selamectin through Caco-2 monolayers shows that Selamectin is P-glycoprotein (P-gp) substrates with a secretory/absorptive ratio of 4.7. Selamectin inhibits the efflux of Rh-123 from peripheral blood lymphocytes (PBL) and the concentration of inhibition is similar to that of Verapamil[2].
A single administration of 6 mg/kg topical Selamectin given every two months could effectively prevent B. malayi infection in cats. Application of topical Selamectin twice a year could block circulating microfilariae[1].
The cats are weighed on Days-2, 29 and 58 to calculate the dosing. Cats in group 1 (control group) remain untreated. On Day 0, the cats in group 3 are treated with fluralaner at the minimum recommending label dose of 40.0 mg per kg body weight. On Days 0, 30 and 60, the cats in group 2 are treated with the new spot-on formulation at the minimum recommending label dose of 1.0 mg/kg sarolaner and 6.0 mg/kg Selamectin. The cats are observed at different time points after treatment for possible adverse reactions to treatment. On Day 0, administration site observations are performed on all cats 30 min (±5 min), 3 h (±15 min) and 24 h (±1 h) and again on Days 3 and 5 after treatment[1].
| | | |
| | | | | |
[1]. Patsharaporn T Sarasombath, et al. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr
118(4):1289-1297. [Content Brief]
[2]. J Griffin, et al. Selamectin is a potent substrate and inhibitor of human and canine P-glycoprotein. J Vet Pharmacol Ther. 2005 Jun
28(3):257-65. [Content Brief]