Fluralaner

Fluralaner is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker [3H]4'-ethynyl-4-n-propylbicycloorthobenzoate (EBOB) to housefly head membranes, with an IC50 value of 455 pM as compared to an IC50 value of >10 µM for rat brain membranes. Fluralaner blocks GABA- and glutamate-induced chloride currents in Xenopus oocytes expressing housefly MdGBCl or MdGluCl channels (IC50s = 5.32 and 79.9 nM, respectively) but has no effect on rat GABA Cl channels (IC50 = >30,000 nM). It has insecticidal and acaricidal activity against C. felis, S. calcitrans, L. cuprina, A. aegypti, R. microplus, R. sanguineus, and O. moubata at concentrations of 0.0000012 to 1 ppm. Formulations containing fluralaner have been used in the prevention and treatment of parasitic infections in veterinary medicine.Formal Name: 4-[5-(3,5-dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-2-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-benzamide. CAS Number: 864731-61-3. Synonyms: A-1443, AH 252723. Molecular Formula: C22H17Cl2F6N3O3. Formula Weight: 556.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml. lambdamax: 265 nm. SMILES: CC1=CC(C2=NOC(C3=CC(Cl)=CC(Cl)=C3)(C(F)(F)F)C2)=CC=C1C(NCC(NCC(F)(F)F)=O)=O. InChi Code: InChI=1S/C22H17Cl2F6N3O3/c1-11-4-12(2-3-16(11)19(35)31-9-18(34)32-10-21(25,26)27)17-8-20(36-33-17,22(28,29)30)13-5-14(23)7-15(24)6-13/h2-7H,8-10H2,1H3,(H,31,35)(H,32,34). InChi Key: MLBZKOGAMRTSKP-UHFFFAOYSA-N.