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MedKoo Cat#: 319689 | Name: Afoxolaner
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Afoxolaner is a potent isoxazoline insecticide/acaricide, against Ixodes scapularis in dogs. 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.

Chemical Structure

Afoxolaner
CAS#1093861-60-9 (Afoxolaner)

Theoretical Analysis

MedKoo Cat#: 319689

Name: Afoxolaner

CAS#: 1093861-60-9 (Afoxolaner)

Chemical Formula: C26H17ClF9N3O3

Exact Mass: 625.0815

Molecular Weight: 625.88

Elemental Analysis: C, 49.90; H, 2.74; Cl, 5.66; F, 27.32; N, 6.71; O, 7.67

Price and Availability

Size Price Availability Quantity
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
1g USD 4,250.00 2 Weeks
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Related CAS #
1093861-60-9 (Afoxolaner) 1096103-99-9 (Esafoxolaner)
Synonym
Afoxolaner, Trade name: NexGard.
IUPAC/Chemical Name
4-(5-(3-Chloro-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)naphthalene-1-carboxamide
InChi Key
OXDDDHGGRFRLEE-UHFFFAOYSA-N
InChi Code
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)
SMILES Code
O=C(C1=C2C=CC=CC2=C(C3=NOC(C(F)(F)F)(C4=CC(C(F)(F)F)=CC(Cl)=C4)C3)C=C1)NCC(NCC(F)(F)F)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 625.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Rehbein S, Fourie JJ, de Vos C, Anderson A, Larsen DL, Jeannin P. Efficacy of oral afoxolaner plus milbemycin oxime chewables against induced infestations with Dermacentor reticulatus in dogs. Parasitol Res. 2016 Jan 27. [Epub ahead of print] PubMed PMID: 26815036. 2: Snyder DE, Rumschlag AJ, Young LM, Ryan WG. Speed of flea knockdown of spinosad compared to afoxolaner, and of spinosad through 28 days post-treatment in controlled laboratory studies. Parasit Vectors. 2015 Nov 9;8:578. doi: 10.1186/s13071-015-1195-5. PubMed PMID: 26552479; PubMed Central PMCID: PMC4640350. 3: Ohmes CM, Hostetler J, Davis WL, Settje T, Everett WR. Comparative Efficacy of an Imidacloprid/Flumethrin Collar (Seresto®) and an Oral Afoxolaner Chewable (NexGard®) against Tick (Dermacentor variabilis and Amblyomma americanum) Infestations on Dogs: a Randomised Controlled Trial. Parasitol Res. 2015 Aug;114 Suppl 1:S81-94. doi: 10.1007/s00436-015-4515-y. PubMed PMID: 26152410. 4: Emmerich IU. [New drugs for small animals in 2014]. Tierarztl Prax Ausg K Kleintiere Heimtiere. 2015;43(3):170-80. doi: 10.15654/TPK-150260. Epub 2015 May 27. German. PubMed PMID: 26013709. 5: Dryden MW, Smith V, Chwala M, Jones E, Crevoiserat L, McGrady JC, Foley KM, Patton PR, Hawkins A, Carithers D. Evaluation of afoxolaner chewables to control flea populations in naturally infested dogs in private residences in Tampa FL, USA. Parasit Vectors. 2015 May 24;8:286. doi: 10.1186/s13071-015-0897-z. PubMed PMID: 26003175; PubMed Central PMCID: PMC4445572. 6: Beugnet F, Liebenberg J, Halos L. Comparative efficacy of two oral treatments for dogs containing either afoxolaner or fluralaner against Rhipicephalus sanguineus sensu lato and Dermacentor reticulatus. Vet Parasitol. 2015 Apr 15;209(1-2):142-5. doi: 10.1016/j.vetpar.2015.02.002. Epub 2015 Feb 12. PubMed PMID: 25716658. 7: Beugnet F, Liebenberg J, Halos L. Comparative speed of efficacy against Ctenocephalides felis of two oral treatments for dogs containing either afoxolaner or fluralaner. Vet Parasitol. 2015 Jan 30;207(3-4):297-301. doi: 10.1016/j.vetpar.2014.12.007. Epub 2014 Dec 19. PubMed PMID: 25564276. 8: Halos L, Lebon W, Chalvet-Monfray K, Larsen D, Beugnet F. Immediate efficacy and persistent speed of kill of a novel oral formulation of afoxolaner (NexGardTM) against induced infestations with Ixodes ricinus ticks. Parasit Vectors. 2014 Sep 26;7:452. doi: 10.1186/1756-3305-7-452. PubMed PMID: 25261196; PubMed Central PMCID: PMC4262065. 9: Beugnet F, deVos C, Liebenberg J, Halos L, Fourie J. Afoxolaner against fleas: immediate efficacy and resultant mortality after short exposure on dogs. Parasite. 2014;21:42. doi: 10.1051/parasite/2014045. Epub 2014 Aug 25. PubMed PMID: 25148564; PubMed Central PMCID: PMC4141545. 10: Beugnet F, Halos L, Larsen D, Labuschagné M, Erasmus H, Fourie J. The ability of an oral formulation of afoxolaner to block the transmission of Babesia canis by Dermacentor reticulatus ticks to dogs. Parasit Vectors. 2014 Jun 23;7:283. doi: 10.1186/1756-3305-7-283. PubMed PMID: 24957215; PubMed Central PMCID: PMC4078974. 11: Kunkle BN, Drag MD, Chester TS, Larsen DL. Assessment of the onset of action of afoxolaner against existing adult flea (Ctenocephalides felis) infestations on dogs. Vet Parasitol. 2014 Apr 2;201(3-4):204-6. doi: 10.1016/j.vetpar.2014.02.023. Epub 2014 Mar 29. PubMed PMID: 24685322. 12: Mitchell EB, McCall JW, Theodore Chester S, Larsen D. Efficacy of afoxolaner against Ixodes scapularis ticks in dogs. Vet Parasitol. 2014 Apr 2;201(3-4):223-5. doi: 10.1016/j.vetpar.2014.02.015. Epub 2014 Mar 29. PubMed PMID: 24685321. 13: Letendre L, Huang R, Kvaternick V, Harriman J, Drag M, Soll M. The intravenous and oral pharmacokinetics of afoxolaner used as a monthly chewable antiparasitic for dogs. Vet Parasitol. 2014 Apr 2;201(3-4):190-7. doi: 10.1016/j.vetpar.2014.02.021. Epub 2014 Mar 29. PubMed PMID: 24685320. 14: Dumont P, Gale B, Chester TS, Larsen DL. Curative and preventive efficacy of orally administered afoxolaner against Ctenocephalides canis infestation in dogs. Vet Parasitol. 2014 Apr 2;201(3-4):212-5. doi: 10.1016/j.vetpar.2014.02.014. Epub 2014 Mar 14. PubMed PMID: 24631503. 15: Shoop WL, Hartline EJ, Gould BR, Waddell ME, McDowell RG, Kinney JB, Lahm GP, Long JK, Xu M, Wagerle T, Jones GS, Dietrich RF, Cordova D, Schroeder ME, Rhoades DF, Benner EA, Confalone PN. Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs. Vet Parasitol. 2014 Apr 2;201(3-4):179-89. doi: 10.1016/j.vetpar.2014.02.020. Epub 2014 Mar 14. PubMed PMID: 24631502. 16: Drag M, Saik J, Harriman J, Larsen D. Safety evaluation of orally administered afoxolaner in 8-week-old dogs. Vet Parasitol. 2014 Apr 2;201(3-4):198-203. doi: 10.1016/j.vetpar.2014.02.022. Epub 2014 Mar 13. PubMed PMID: 24629431. 17: Otranto D. NEXGARD®. Afoxolaner, a new oral insecticide-acaricide to control fleas and ticks in dogs. Editorial. Vet Parasitol. 2014 Apr 2;201(3-4):177-8. doi: 10.1016/j.vetpar.2014.02.029. Epub 2014 Mar 12. PubMed PMID: 24629430. 18: Kondo Y, Kinoshita G, Drag M, Chester TS, Larsen D. Evaluation of the efficacy of afoxolaner against Haemaphysalis longicornis on dogs. Vet Parasitol. 2014 Apr 2;201(3-4):229-31. doi: 10.1016/j.vetpar.2014.02.019. Epub 2014 Mar 13. PubMed PMID: 24629429. 19: Mitchell EB, Dorr P, Everett WR, Chester TS, Larsen D. Efficacy of afoxolaner against Dermacentor variabilis ticks in dogs. Vet Parasitol. 2014 Apr 2;201(3-4):220-2. doi: 10.1016/j.vetpar.2014.02.016. Epub 2014 Mar 13. PubMed PMID: 24629426. 20: Kunkle B, Daly S, Dumont P, Drag M, Larsen D. Assessment of the efficacy of orally administered afoxolaner against Rhipicephalus sanguineus sensu lato. Vet Parasitol. 2014 Apr 2;201(3-4):226-8. doi: 10.1016/j.vetpar.2014.02.018. Epub 2014 Mar 13. PubMed PMID: 24629425.