Lotilaner CAS# 1369852-71-0

Lotilaner is an isoxazoline ectoparasiticide that acts as a potent inhibitor of γ-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride channels in arthropods. In vitro studies show that Lotilaner exhibits strong activity against Ctenocephalides felis (cat flea) and Rhipicephalus sanguineus (brown dog tick), with IC₅₀ values in the low nanomolar range (typically 3–10 nM) for blocking flea GABA-gated chloride channels, while showing >1000-fold selectivity over mammalian receptors. In cell-based assays, it causes rapid hyperexcitation and death of fleas and ticks. In vivo, oral administration of Lotilaner to dogs (20–40 mg/kg) results in >99% flea and tick mortality within 4–8 hours post-treatment and maintains efficacy (>95%) for at least 30 days. In cat models, a single 6–12 mg/kg oral dose eliminated >98% of flea infestations within 24 hours.