Sarolaner (C09-1169-825)

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 LC 80 value of 0.3 μg/mL against C. felis and a LC 100 value of 0.003 μg/mL against O. turicataIn VitroSarolaner (450 nM-1 mM; 5 min) inhibits CfRDL-A285 and CfRDL-S285 receptors with γ-Aminobutyric acid (GABA)-induced currents. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: CHO-K1 cell lines Concentration: 450 nM-1 mM Incubation Time: 5 min Result: Inhibited GABA-elicited currents at both susceptible (CfRDL-A285) and resistant (CfRDL-S285) flea GABACls with EC 50 s of 135 and 136 nM, respectively.In VivoSarolaner (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Dog infested with R. sanguineus and D. reticulatus Dosage: 2.5 mg/kg Administration: Oral gavage; 2.5 mg/kg once Result: Exibited 100% efficacy against R. sanguineus at 48 hours after treatment and also exhibited 98.0% efficacy against D. reticulatus . Animal Model: Dog infested with I. ricinus Dosage: 1.25, 2.5 and 5 mg/kg Administration: Oral gavage; 1.25, 2.5 and 5 mg/kg once Result: Exibited 100% efficacy against I. ricinus at all doses until 7 days, and provided over 99.3% reduction against subsequent re-infestations until 57 days at dose of 5.0 and 2.5 mg/kg.Form:SolidIC50& Target:LC80: 0.3μg/mL ( C. felis ), LC100: 0.003 μg/mL ( O. turicata ), IC50: 135 nM (CfRDL-A285), 136 nM (CfRDL-S285). Specification: 0.99 Molecular Formula: C23H18Cl2F4N2O5S Molecular Weight: 581.36 PubChem CID: 73169092 Isomeric SMILES: 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