Afoxolaner

Names

[ Name ]:
Afoxolaner

[Synonym ]:
4-[(5R)-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
4-[(5RS)-5-(5-chloro-α,α,α-trifluoro-m-tolyl)-4,5-dihydro-5-(trifluoromethyl)-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
UNII-02L07H6D0U
rac-4-{(5R)-5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4,5-dihydro-1,2-oxazol-3-yl}-N-{2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl}naphthalene-1-carboxamide
4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide
Afoxolaner

Biological Activity

[Description]:

Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Chloride Channel

Research Areas >> Infection

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vivo]

A single oral treatment with a dose approaching the minimum effective dose of afoxolaner (2.5mg/kg) eliminated the pre-existing infestations of I. scapularis ticks and controlled weekly re-infestations, with efficacy between 98% and 100% recorded until Day 23 and 94% at Day 30[1].

[References]

[1]. Mitchell EB, et al. Efficacy of afoxolaner against Ixodes scapularis ticks in dogs.Vet Parasitol. 2014 Apr 2;201(3-4):223-5.

[2]. Beugnet F, et al. Afoxolaner against fleas: immediate efficacy and resultant mortality after short exposure on dogs.Parasite. 2014;21:42.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₁₇ClF₉N₃O₃

[ Molecular Weight ]:
625.87000

[ Exact Mass ]:
625.08100

[ PSA ]:
79.79000

[ LogP ]:
6.71990