MedKoo Cat#: 319659 | Name: Lotilaner
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Description:

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

Lotilaner is an insecticide (veterinary drug). Lotilaner acts as a potent non-competitive antagonist of insects GABACl receptors. Lotilaner efficacy was 100% within 48 h post-treatment, and at nine days post-treatment. Efficacy was greater than 99% at all subsequent assessments through Day 30. No treatment-related adverse events were observed.

Chemical Structure

Lotilaner
Lotilaner
CAS#1369852-71-0

Theoretical Analysis

MedKoo Cat#: 319659

Name: Lotilaner

CAS#: 1369852-71-0

Chemical Formula: C20H14Cl3F6N3O3S

Exact Mass: 594.9726

Molecular Weight: 596.75

Elemental Analysis: C, 40.25; H, 2.36; Cl, 17.82; F, 19.10; N, 7.04; O, 8.04; S, 5.37

Price and Availability

Size Price Availability Quantity
5mg USD 550.00 2 Weeks
10mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
Lotilaner, Credelio,
IUPAC/Chemical Name
(S)-3-methyl-N-(2-oxo-2-((2,2,2-trifluoroethyl)amino)ethyl)-5-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)thiophene-2-carboxamide
InChi Key
HDKWFBCPLKNOCK-SFHVURJKSA-N
InChi Code
InChI=1S/C20H14Cl3F6N3O3S/c1-8-2-13(36-16(8)17(34)30-6-14(33)31-7-19(24,25)26)12-5-18(35-32-12,20(27,28)29)9-3-10(21)15(23)11(22)4-9/h2-4H,5-7H2,1H3,(H,30,34)(H,31,33)/t18-/m0/s1
SMILES Code
O=C(C1=C(C)C=C(C2=NO[C@](C(F)(F)F)(C3=CC(Cl)=C(Cl)C(Cl)=C3)C2)S1)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 596.75 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: Fuatos Gámez BA, Sánchez Cisneros JS, Villarreal Villarreal JP, Miranda Contreras L, Romero Núñez C. Effectiveness of lotilaner against ticks of the genus Amblyomma spp. in three naturally infested cane toads (Rhinella horribilis). Vet Dermatol. 2021 Nov 14. doi: 10.1111/vde.13043. Epub ahead of print. PMID: 34779052. 2: Gonzalez-Salinas R, Yeu E, Holdbrook M, Baba SN, Ceballos JC, Massaro- Corredor M, Corredor-Ortega C, Ramos-Betancourt N, Quiroz-Mercado H. Safety and Efficacy of Topical Lotilaner Ophthalmic Solution 0.25% for the Treatment of Demodex Blepharitis: A Pilot Study. J Ophthalmol. 2021 Sep 21;2021:3862684. doi: 10.1155/2021/3862684. PMID: 34603770; PMCID: PMC8481060. 3: Gonzalez-Salinas R, Yeu E, Holdbrook M, Baba SN, Ceballos JC, Massaro- Corredor M, Corredor-Ortega C, Ramos-Betancourt N, Quiroz-Mercado H. Collarette Elimination and Demodex Mite Eradication with Topical Lotilaner Ophthalmic Solution, 0.25. J Ocul Pharmacol Ther. 2021 Oct;37(8):479-484. doi: 10.1089/jop.2021.0011. Epub 2021 Aug 20. PMID: 34415795. 4: Salinas RG, Karpecki P, Yeu E, Holdbrook M, Baba SN, Ceballos JC, Massaro- Corredor M, Corredor-Ortega C, Ramos-Betancourt N, Quiroz-Mercado H. Safety and efficacy of lotilaner ophthalmic solution, 0.25% for the treatment of blepharitis due to demodex infestation: A randomized, controlled, double-masked clinical trial. Cont Lens Anterior Eye. 2021 Jul 28:101492. doi: 10.1016/j.clae.2021.101492. Epub ahead of print. PMID: 34332895. 5: Wenger MJ, Kollasch TM, Burke MC, Jones L, Locklear C, Hedberg M, Miller L, Reeves S, Ritchie D, Rumschlag AJ, Ryan WG, Smith V, Sutherland C, Reif KE, Herrin BH. Early onset of pre-lethal effects of lotilaner (Credelio®) on Amblyomma americanum ticks on experimentally infested dogs. Parasit Vectors. 2021 Jun 13;14(1):322. doi: 10.1186/s13071-021-04817-z. PMID: 34120646; PMCID: PMC8201672. 6: Forster S, Wiseman S, Snyder DE. Field study to investigate the effectiveness and safety of a novel orally administered combination drug product containing milbemycin oxime and lotilaner (Credelio® Plus) against natural flea and tick infestations on dogs presented as veterinary patients in Europe. Parasit Vectors. 2021 Jun 4;14(1):299. doi: 10.1186/s13071-021-04808-0. PMID: 34088338; PMCID: PMC8178840. 7: Traversa D. Credelio® Plus: a novel oral endectocide for dogs. Parasit Vectors. 2021 May 28;14(1):286. doi: 10.1186/s13071-021-04774-7. PMID: 34044877; PMCID: PMC8161950. 8: Young LM, Wiseman S, Crawley E, Wallace K, Snyder DE. Field study to investigate the effectiveness and safety of a novel orally administered combination drug product containing milbemycin oxime and lotilaner (Credelio® Plus) for the prevention of heartworm disease (Dirofilaria immitis) in client-owned dogs in the USA. Parasit Vectors. 2021 May 28;14(1):284. doi: 10.1186/s13071-021-04767-6. PMID: 34044864; PMCID: PMC8161898. 9: Riggs KL, Wiseman S. Long-term and acute safety of a novel orally administered combination drug product containing milbemycin oxime and lotilaner (Credelio® Plus) in juvenile and adult dogs. Parasit Vectors. 2021 May 28;14(1):285. doi: 10.1186/s13071-021-04760-z. PMID: 34044853; PMCID: PMC8161958. 10: Young LM, Wiseman S, Crawley E, Bowman DD, Reinemeyer CR, Snyder DE. Effectiveness of Credelio® Plus, a novel chewable tablet containing milbemycin oxime and lotilaner for the treatment of larval and immature adult stages of Toxocara canis in experimentally infected dogs. Parasit Vectors. 2021 May 17;14(1):256. doi: 10.1186/s13071-021-04762-x. PMID: 34001224; PMCID: PMC8127296. 11: Hayes B, Wiseman S, Snyder DE. Field study to investigate the effectiveness and safety of a novel orally administered combination drug product containing milbemycin oxime and lotilaner (Credelio® Plus) against natural intestinal nematode infections in dogs presented as veterinary patients in Europe. Parasit Vectors. 2021 May 17;14(1):258. doi: 10.1186/s13071-021-04766-7. PMID: 34001223; PMCID: PMC8127225. 12: Snyder DE, Wiseman S, Crawley E, Wallace K, Bowman DD, Reinemeyer CR. Effectiveness of a novel orally administered combination drug product containing milbemycin oxime and lotilaner (Credelio® Plus) for the treatment of larval and immature adult stages of Ancylostoma caninum in experimentally infected dogs. Parasit Vectors. 2021 May 17;14(1):255. doi: 10.1186/s13071-021-04761-y. PMID: 34001200; PMCID: PMC8127199. 13: Zhou X, Hohman AE, Hsu WH. Current review of isoxazoline ectoparasiticides used in veterinary medicine. J Vet Pharmacol Ther. 2021 Mar 17. doi: 10.1111/jvp.12959. Epub ahead of print. PMID: 33733534. 14: Paarlberg T, Karadzovska D, Helbig R. Efficacy of lotilaner (Credelio™) against experimentally induced infestations of the adult cat flea, Ctenocephalides felis, and flea eggs following oral administration to cats. Parasit Vectors. 2021 Mar 5;14(1):139. doi: 10.1186/s13071-021-04660-2. PMID: 33673848; PMCID: PMC7934462. 15: Chappell K, Paarlberg T, Seewald W, Karadzovska D, Nanchen S. A randomized, controlled field study to assess the efficacy and safety of lotilaner flavored chewable tablets (Credelio™ CAT) in eliminating fleas in client-owned cats in the USA. Parasit Vectors. 2021 Mar 1;14(1):127. doi: 10.1186/s13071-021-04617-5. PMID: 33648556; PMCID: PMC7923547. 16: Lamassiaude N, Toubate B, Neveu C, Charnet P, Dupuy C, Debierre-Grockiego F, Dimier-Poisson I, Charvet CL. The molecular targets of ivermectin and lotilaner in the human louse Pediculus humanus humanus: New prospects for the treatment of pediculosis. PLoS Pathog. 2021 Feb 18;17(2):e1008863. doi: 10.1371/journal.ppat.1008863. PMID: 33600484; PMCID: PMC7891696. 17: Moog F, Brun J, Bourdeau P, Cadiergues MC. Clinical, Parasitological, and Serological Follow-Up of Dogs with Sarcoptic Mange Treated Orally with Lotilaner. Case Rep Vet Med. 2021 Jan 25;2021:6639017. doi: 10.1155/2021/6639017. PMID: 33575060; PMCID: PMC7857930. 18: Han HS, Yasmin L. Chrysomya bezziana (Diptera: Calliphoridae) infestation in two Malaysian cats treated with oral lotilaner. Vet Dermatol. 2020 Aug;31(4):335-e87. doi: 10.1111/vde.12855. Epub 2020 Apr 22. PMID: 32323413. 19: Young L, Karadzovska D, Wiseman S, Helbig R. Efficacy of lotilaner (Credelio™) against the adult cat flea, Ctenocephalides felis and flea eggs following oral administration to dogs. Parasit Vectors. 2020 Jan 14;13(1):25. doi: 10.1186/s13071-019-3873-1. PMID: 31937370; PMCID: PMC6961367. 20: Emmerich IU. Neue Arzneimittel für Kleintiere 2018 [New drugs for small animals in 2018]. Tierarztl Prax Ausg K Kleintiere Heimtiere. 2019 Apr;47(2):112-118. German. doi: 10.1055/a-0858-4261. Epub 2019 Apr 23. PMID: 31013528.