Sarolaner

Sarolaner is an isoxazoline ectoparasiticide. It inhibits GABA-induced chloride currents in CHO-K1 cells expressing either the gene for susceptible C. felis flea resistance-to-dieldrin subunits containing alanine at residue 285 (CfRDL-A285, IC50 = 135 nM) or the gene for CfRDL subunits containing the alanine-to-serine resistance mutation (CfRDL-S285, IC50 = 136 nM). It induces mortality in C. felis fleas (LC80 = 0.3 µg/ml) and O. turicata soft ticks (LC100 = 0.003 µg/ml). Sarolaner (2.5 mg/kg) eliminates live C. felis fleas, as well as R. sanguineus, I. ricinus, and D. reticulatus ticks, on dogs after 48 hours and reduces the number of fleas and ticks for at least 35 days. Formulations containing sarolaner have been used in the treatment and control of flea and tick infestations in dogs.Formal Name: 1-[5'-[(5S)-5-(3,5-dichloro-4-fluorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]spiro[azetidine-3,1'(3'H)-isobenzofuran]-1-yl]-2-(methylsulfonyl)-ethanone. CAS Number: 1398609-39-6. Synonyms: PF-6450567. Molecular Formula: C23H18Cl2F4N2O5S. Formula Weight: 581.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: Slightly soluble, DMSO: Slightly soluble, Ethanol: Slightly soluble. lambdamax: 261 nm. SMILES: CS(CC(N1CC2(C1)C3=CC=C(C4=NO[C@](C(F)(F)F)(C5=CC(Cl)=C(C(Cl)=C5)F)C4)C=C3CO2)=O)(=O)=O. InChi Code: InChI=1S/C23H18Cl2F4N2O5S/c1-37(33,34)9-19(32)31-10-21(11-31)15-3-2-12(4-13(15)8-35-21)18-7-22(36-30-18,23(27,28)29)14-5-16(24)20(26)17(25)6-14/h2-6H,7-11H2,1H3/t22-/m0/s1. InChi Key: FLEFKKUZMDEUIP-QFIPXVFZSA-N.