Afoxolaner

• CAT Number: I001327
• CAS Number: 1093861-60-9
• Molecular Formula: C26H17ClF9N3O3
• Molecular Weight: 625.876
• Purity: ≥95%
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°Cfor short term (days to weeks), or -20 °C for long term (months).
• IUPAC Name: 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
• InChI: InChI=1S/C26H17ClF9N3O3/c27-15-8-13(7-14(9-15)25(31,32)33)23(26(34,35)36)10-20(39-42-23)18-5-6-19(17-4-2-1-3-16(17)18)22(41)37-11-21(40)38-12-24(28,29)30/h1-9H,10-12H2,(H,37,41)(H,38,40)
• InChIKey: OXDDDHGGRFRLEE-UHFFFAOYSA-N
• SMILES: C1C(=NOC1(C2=CC(=CC(=C2)Cl)C(F)(F)F)C(F)(F)F)C3=CC=C(C4=CC=CC=C43)C(=O)NCC(=O)NCC(F)(F)F

Afoxolaner (Cat No.:I001327) is the first oral dewormer for dogs in China that kills both ticks and fleas. It belongs to the isoxazoline family, and is a revolutionary and potent dewormer that inhibits the GABA chloride channel, causing high neural excitation in arthropods, resulting in death.

Reference

1:Efficacy of afoxolaner plus milbemycin oxime chewable tablets (NexGard Spectra®, Merial) against adult Ancylostoma ceylanicum hookworm, in dogs. Tielemans E, Lebon W, Dumont P, Taweethavonsawat P, Larsen D, Rehbein S.Vet Parasitol. 2017 Apr 30;238:87-89. doi: 10.1016/j.vetpar.2017.03.028. Epub 2017 Apr 1. PMID: 28408213
2:Comparative speed of kill of sarolaner (Simparica®) and afoxolaner (NexGard®) against induced infestations of Ixodes holocyclus on dogs. Packianathan R, Hodge A, Bruellke N, Davis K, Maeder S.Parasit Vectors. 2017 Feb 21;10(1):98. doi: 10.1186/s13071-017-2024-9. PMID: 28222813 Free PMC Article
3:Assessment of afoxolaner efficacy against Otodectes cynotis infestations of dogs. Carithers D, Crawford J, de Vos C, Lotriet A, Fourie J.Parasit Vectors. 2016 Dec 9;9(1):635. PMID: 27938395 Free PMC Article
4:A comparative laboratory trial evaluating the immediate efficacy of fluralaner, afoxolaner, sarolaner and imidacloprid + permethrin against adult Rhipicephalus sanguineus (sensu lato) ticks attached to dogs. Burgio F, Meyer L, Armstrong R.Parasit Vectors. 2016 Dec 3;9(1):626. PMID: 27912787 Free PMC Article
5:Development and Validation of a Normal Phase Chiral HPLC Method for Analysis of Afoxolaner Using a Chiralpak® AD-3 Column. Zhuang J, Kumar S, Rustum A.J Chromatogr Sci. 2016 Nov;54(10):1813-1819. Epub 2016 Oct 7. PMID: 27908928
6:Safety evaluation of orally administered afoxolaner and milbemycin oxime in eight-week-old dogs. Drag M, Saik J, Harriman J, Letendre L, Yoon S, Larsen D.J Vet Pharmacol Ther. 2016 Nov 27. doi: 10.1111/jvp.12375. [Epub ahead of print] PMID: 27891622
7:Ability of an oral formulation of afoxolaner to protect dogs from Borrelia burgdorferi infection transmitted by wild Ixodes scapularis ticks. Baker CF, McCall JW, McCall SD, Drag MD, Mitchell EB, Chester ST, Larsen D.Comp Immunol Microbiol Infect Dis. 2016 Dec;49:65-69. doi: 10.1016/j.cimid.2016.09.004. Epub 2016 Sep 29. PMID: 27865266 Free Article
8:Efficacy against nematode infections and safety of afoxolaner plus milbemycin oxime chewable tablets in domestic dogs under field conditions in Europe. Rehbein S, Knaus M, Mallouk Y, Breiltgens T, Brianti E, Capári B, Dantas-Torres F, Gau M, Joachim A, Kaulfuß KH, Kirkova Z, Lechner J, Mihalca AD, Mirabito R, Petkevičius S, Rapti D, Shukullari E, Sedeilhan M, Dollhofer D, Kley K, Lebon W, Visser M, Jeannin P.Parasitol Res. 2017 Jan;116(1):259-269. Epub 2016 Oct 22. PMID: 27771803
9:Development and Validation of a Reversed-Phase Chiral HPLC Method to Determine the Chiral Purity of Bulk Batches of (S)-Enantiomer in Afoxolaner. Kumar S, Rustum A, Padivitage N.J AOAC Int. 2016 Oct 13. [Epub ahead of print] PMID: 27743445
10:The intravenous and oral pharmacokinetics of afoxolaner and milbemycin oxime when used as a combination chewable parasiticide for dogs. Letendre L, Harriman J, Drag M, Mullins A, Malinski T, Rehbein S.J Vet Pharmacol Ther. 2017 Jan;40(1):35-43. doi: 10.1111/jvp.12332. Epub 2016 Sep 7. PMID: 27604405