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afoxolaner

afoxolaner structure

CAS No:
1093861-60-9
Formula:
C26H17ClF9N3O3
Chemical Name:
afoxolaner
Synonyms:
Afoxolaner;1-Naphthalenecarboxamide, 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-;afoxolaner-007;China biggest manufacturer,Afoxolaner,1093861-60-9;4-(5-(3-Chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-1-naphthamide;Avrana;Afulana;C10047600 Afoxolaner
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Afoxolaner is an insecticide and acaricide belonging to the isoxazoline family. Afoxolaner acts at ligand-gated chloride channels, in particular those gated by the neurotransmitter gamma-aminobutyric acid (GABA), thereby blocking pre- and post-synaptic transfer of chloride ions across cell membranes.

Afoxolaner is used to treat and control flea and tick infestations in dogs. After being ingested by a dog, afoxolaner is distributed throughout the dog’s body. When fleas or ticks bite the dog, they are exposed to the drug and killed during their blood meal.

afoxolaner Basic Attributes

Molecular Weight：

625.87

Exact Mass：

625.87

EC Number：

200-001-8

DSSTox ID：

DTXSID50148921

Color/Form：

White to off-white

ATC Code：

QP53BE01|QP54AB51

Characteristics

Density：

1.53±0.1 g/cm3(Predicted)

PKA：

12.45±0.46(Predicted)

Critical Temperature & Pressure：

Store at -20°C

Safety Information

GHS Classification：

|Warning|H361 (97.22%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P273, P281, P308+P313, P391, P405, and P501|Aggregated GHS information provided by 36 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Treatment of flea (Ctenocephalides felis and C. canis) infestations. The product can be used as part of a treatment strategy for the control of flea allergy dermatitis (FAD)., , Treatment of tick (Dermacentor reticulatus, Ixodes ricinus, Rhipicephalus sanguineus) infestations., , Treatment of demodicosis (caused by Demodex canis)., , Treatment of sarcoptic mange (caused by Sarcoptes scabiei var. canis).,|For the treatment of flea and tick infestations in dogs when the concurrent prevention of heartworm disease (Dirofilaria immitis larvae), angiostrongylosis (reduction in level of immature adults (L5) and adults of Angiostrongylus vasorum), thelaziosis (adult Thelazia callipaeda) and/or treatment of gastrointestinal nematode infestations is indicated.Treatment of flea infestations (Ctenocephalides felis and C. canis) in dogs for 5 weeks. Treatment of tick infestations (Dermacentor reticulatus, Ixodes ricinus, Ixodes hexagonus, Rhipicephalus sanguineus) in dogs for 4 weeks.Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance.Treatment of infestations with adult gastrointestinal nematodes of the following species: roundworms (Toxocara canis and Toxascaris leonina), hookworms (Ancylostoma caninum, Ancylostoma braziliense and Ancylostoma ceylanicum) and whipworm (Trichuris vulpis). Treatment of demodicosis (caused by Demodex canis). Treatment of sarcoptic mange (caused by Sarcoptes scabiei var. canis). Prevention of heartworm disease (Dirofilaria immitis larvae) with monthly administration. Prevention of angiostrongylosis (by reduction of the level of infection with immature adult (L5) and adult stages of Angiostrongylus vasorum) with monthly administration.Prevention of establishment of thelaziosis (adult Thelazia callipaeda eyeworm infection) with monthly administration.|Treatment of flea infestation in dogs (Ctenocephalides felis and C. canis) for at least 5 weeks. The product can be used as part of a treatment strategy for the control of flea allergy dermatitis (FAD).Treatment of tick infestation in dogs (Dermacentor reticulatus, Ixodes ricinus, Ixodes hexagonus, Rhipicephalus sanguineus). One treatment kills ticks for up to one month.Fleas and ticks must attach to the host and commence feeding in order to be exposed to the active substance. Treatment of demodicosis (caused by Demodex canis).Treatment of sarcoptic mange (caused by Sarcoptes scabiei var. canis).

MeSH Entry Terms：

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 Use and Manufacturing

Uses

Afoxolaner (brand name NexGard®) is used to treat and control flea and tick infestations in dogs. After being ingested by a dog, afoxolaner is distributed throughout the dog's body. When fleas or ticks bite the dog, they are exposed to the drug and killed during their blood meal.

Use Classification：

Veterinary drugs -> Frontpro (previously known as Afoxolaner Merial) -> EMA Drug Category|Ectoparasiticides for systemic use -> Veterinary pharmacotherapeutic group|Veterinary drugs -> Nexgard Spectra -> EMA Drug Category|Endectocides, Antiparasitic products, insecticides and repellents, milbemycin oxime, combinations -> Veterinary pharmacotherapeutic group|Veterinary drugs -> NexGard -> EMA Drug Category|Isoxazolines, Ectoparasiticides for systemic use -> Veterinary pharmacotherapeutic group|Animal Drugs -> FDA Approved Animal Drug Products (Green Book) -> Active Ingredients

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