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.IC50 & Target: LC80: 0.3μg/mL (C. felis)
LC100: 0.003 μg/mL (O. turicata)
IC50: 135 nM (CfRDL-A285), 136 nM (CfRDL-S285)In Vitro: Sarolaner (450 nM-1 mM; 5 min) inhibits CfRDL-A285 and CfRDL-S285 receptors with γ-Aminobutyric acid (GABA)-induced currents.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.