Synonym
Selamectin; Revolution; Stronghold;
IUPAC/Chemical Name
A name could not be generated for this structure.
InChi Key
AFJYYKSVHJGXSN-HFDNCIBQSA-N
InChi Code
InChI=1S/C43H63NO11/c1-24-11-10-14-30-23-50-40-36(44-48)27(4)19-33(43(30,40)47)41(46)52-32-20-31(16-15-25(2)38(24)53-35-21-34(49-6)37(45)28(5)51-35)54-42(22-32)18-17-26(3)39(55-42)29-12-8-7-9-13-29/h10-11,14-15,19,24,26,28-29,31-35,37-40,45,47-48H,7-9,12-13,16-18,20-23H2,1-6H3/b11-10+,25-15+,30-14+,44-36-/t24-,26-,28-,31-,32-,33-,34+,35-,37-,38-,39-,40+,42+,43-/m0/s1
SMILES Code
CC1=C[C@H]([C@]2(O)[C@H](OC/C2=C\C=C\[C@H](C)[C@@H](/C(C)=C/C[C@H](O3)C4)O[C@@H]5O[C@@H](C)[C@@H]([C@@H](C5)OC)O)/C1=N\O)C(O[C@@H]4C[C@]63O[C@H](C7CCCCC7)[C@@H](C)CC6)=O
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, DMF, and ethanol
Shelf Life
>3 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
2934.99.03.00
Biological target:
Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
In vitro activity:
Selamectin may represent a timely and promising macrocyclic lactone for the treatment of S. aureus infections. Selamectin exposure caused relevant cell surface alterations and drug administration at MIC concentration reduced the intracellular bacterial load by 81.3%. Selamectin reduced the biofilm biomass in a dose-dependent manner with minimal biofilm eradication concentrations. Selamectin also exhibited no relevant hemolytic and cytotoxic activity at active concentrations.
Reference: Microorganisms. 2023 Sep 6;11(9):2242. https://pubmed.ncbi.nlm.nih.gov/37764086/
In vivo activity:
This study investigated the chemotherapeutic efficacy of topical selamectin against cats infected with lymphatic filariae (Brugia malayi and Brugia pahangi). Topical selamectin treatment in B. malayi and B. pahangi microfilaremic cats showed 100% effectivity in eradicating microfilaremia but only 78.5% effectivity in eliminating filarial DNA. The findings of this study suggest that topical selamectin could effectively prevent B. malayi infection and could block circulating microfilariae.
Reference: Parasitol Res. 2019 Apr;118(4):1289-1297. https://pubmed.ncbi.nlm.nih.gov/30746583/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
15.0 |
19.48 |
|
| DMSO |
15.0 |
19.48 |
|
| Ethanol |
15.0 |
19.48 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
769.97
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.
| 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 |
Formulation protocol:
1. Folliero V, Dell'Annunziata F, Santella B, Roscetto E, Zannella C, Capuano N, Perrella A, De Filippis A, Boccia G, Catania MR, Galdiero M, Franci G. Repurposing Selamectin as an Antimicrobial Drug against Hospital-Acquired Staphylococcus aureus Infections. Microorganisms. 2023 Sep 6;11(9):2242. doi: 10.3390/microorganisms11092242. PMID: 37764086; PMCID: PMC10535345.
2. Ezquerra-Aznárez JM, Degiacomi G, Gašparovič H, Stelitano G, Sammartino JC, Korduláková J, Governa P, Manetti F, Pasca MR, Chiarelli LR, Ramón-García S. The Veterinary Anti-Parasitic Selamectin Is a Novel Inhibitor of the Mycobacterium tuberculosis DprE1 Enzyme. Int J Mol Sci. 2022 Jan 11;23(2):771. doi: 10.3390/ijms23020771. PMID: 35054958; PMCID: PMC8776228.
3. Taweethavonsawat P, Chaimee T, Priyavoravong P, Traub RJ. Efficacy of single topical treatment of Selamectin (Revolution®) against Ancylostoma ceylanicum in experimentally infected cats. Vet Parasitol Reg Stud Reports. 2019 Dec;18:100346. doi: 10.1016/j.vprsr.2019.100346. Epub 2019 Oct 31. PMID: 31796176.
4. Sarasombath PT, Thammapalo S, Loymek S, Angkanasinsiri A, Priyavoravong P, Wongkamchai S. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr;118(4):1289-1297. doi: 10.1007/s00436-019-06248-3. Epub 2019 Feb 12. Erratum in: Parasitol Res. 2023 Sep;122(9):2243. PMID: 30746583.
In vitro protocol:
1. Folliero V, Dell'Annunziata F, Santella B, Roscetto E, Zannella C, Capuano N, Perrella A, De Filippis A, Boccia G, Catania MR, Galdiero M, Franci G. Repurposing Selamectin as an Antimicrobial Drug against Hospital-Acquired Staphylococcus aureus Infections. Microorganisms. 2023 Sep 6;11(9):2242. doi: 10.3390/microorganisms11092242. PMID: 37764086; PMCID: PMC10535345.
2. Ezquerra-Aznárez JM, Degiacomi G, Gašparovič H, Stelitano G, Sammartino JC, Korduláková J, Governa P, Manetti F, Pasca MR, Chiarelli LR, Ramón-García S. The Veterinary Anti-Parasitic Selamectin Is a Novel Inhibitor of the Mycobacterium tuberculosis DprE1 Enzyme. Int J Mol Sci. 2022 Jan 11;23(2):771. doi: 10.3390/ijms23020771. PMID: 35054958; PMCID: PMC8776228.
In vivo protocol:
1. Taweethavonsawat P, Chaimee T, Priyavoravong P, Traub RJ. Efficacy of single topical treatment of Selamectin (Revolution®) against Ancylostoma ceylanicum in experimentally infected cats. Vet Parasitol Reg Stud Reports. 2019 Dec;18:100346. doi: 10.1016/j.vprsr.2019.100346. Epub 2019 Oct 31. PMID: 31796176.
2. Sarasombath PT, Thammapalo S, Loymek S, Angkanasinsiri A, Priyavoravong P, Wongkamchai S. First study of topical selamectin efficacy for treating cats naturally infected with Brugia malayi and Brugia pahangi under field conditions. Parasitol Res. 2019 Apr;118(4):1289-1297. doi: 10.1007/s00436-019-06248-3. Epub 2019 Feb 12. Erratum in: Parasitol Res. 2023 Sep;122(9):2243. PMID: 30746583.
1: Moraes-da-Silva Mde F, Mendes-de-Almeida F, Abdalla L, Merlo A, Paiva JP, Labarthe NV. Selamectin for the prevention of canine Dirofilaria immitis infection: field efficacy in client-owned dogs in a high risk area. Parasit Vectors. 2016 Jul 22;9(1):407. doi: 10.1186/s13071-016-1697-9. PubMed PMID: 27450482; PubMed Central PMCID: PMC4957884.
2: Robinson N, Brennan M. Selamectin versus ivermectin for cheyletiellosis in pet rabbits. Vet Rec. 2016 Apr 2;178(14):344-5. doi: 10.1136/vr.i1387. PubMed PMID: 27034299.
3: Scherr N, Pluschke G, Thompson CJ, Ramón-García S. Selamectin Is the Avermectin with the Best Potential for Buruli Ulcer Treatment. PLoS Negl Trop Dis. 2015 Aug 13;9(8):e0003996. doi: 10.1371/journal.pntd.0003996. eCollection 2015 Aug. PubMed PMID: 26270480; PubMed Central PMCID: PMC4536011.
4: Bouhsira E, Franc M, Lienard E, Bouillin C, Gandoin C, Geurden T, Becskei C, Jacquiet P, Thomas A, Boulouis HJ. The efficacy of a selamectin (Stronghold ®) spot on treatment in the prevention of Bartonella henselae transmission by Ctenocephalides felis in cats, using a new high-challenge model. Parasitol Res. 2015 Mar;114(3):1045-50. doi: 10.1007/s00436-014-4271-4. Epub 2015 Jan 14. PubMed PMID: 25582566; PubMed Central PMCID: PMC4336412.
5: Hahn A, D'Agostino J, Cole G, Kukanich B. Pharmacokinetics of selamectin in helmeted guineafowl (Numida meleagris) after topical administration. J Zoo Wildl Med. 2014 Mar;45(1):176-8. PubMed PMID: 24712181.
6: Bozzatto V, Oliveira PR, Bechara GH, Camargo-Mathias MI. Morphological alterations of epidermis of rabbits infested by R. sanguineus ticks and exposed to Selamectin (active principle of Pfizer Revolution(®) acaricide): a confocal microscopy study. Acta Histochem. 2014 Apr;116(3):534-8. doi: 10.1016/j.acthis.2013.11.011. Epub 2013 Dec 23. PubMed PMID: 24369880.
7: Bozzatto V, Oliveira PR, Furquim KC, Camargo-Mathias MI. The occurrence of autophagic cell death in the tegument of rabbits pre-infested with Rhipicephalus sanguineus and exposed to selamectin (active principle of acaricide Pfizer Revolution®). Microsc Res Tech. 2013 Nov;76(11):1171-6. doi: 10.1002/jemt.22281. Epub 2013 Aug 23. PubMed PMID: 23983162.
8: Dryden MW, Payne PA, Smith V, Berg TC, Lane M. Efficacy of selamectin, spinosad, and spinosad/milbemycin oxime against the KS1 Ctenocephalides felis flea strain infesting dogs. Parasit Vectors. 2013 Mar 25;6:80. doi: 10.1186/1756-3305-6-80. PubMed PMID: 23531322; PubMed Central PMCID: PMC3621083.
9: Eshar D, Bdolah-Abram T. Comparison of efficacy, safety, and convenience of selamectin versus ivermectin for treatment of Trixacarus caviae mange in pet guinea pigs (Cavia porcellus). J Am Vet Med Assoc. 2012 Oct 15;241(8):1056-8. doi: 10.2460/javma.241.8.1056. PubMed PMID: 23039980.
10: Carpenter JW, Dryden MW, Kukanich B. Pharmacokinetics, efficacy, and adverse effects of selamectin following topical administration in flea-infested rabbits. Am J Vet Res. 2012 Apr;73(4):562-6. doi: 10.2460/ajvr.73.4.562. PubMed PMID: 22452505.
