Doramectin | CAS#117704-25-3 | antiparasitic drug

MedKoo Cat#: 561486 | Name: Doramectin

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Description:

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

Doramectin is a macrocyclic lactone antiparasitic that targets glutamate-gated chloride channels (GluCl) in nematodes and arthropods, causing paralysis and death of the parasite. It has a broad spectrum of activity against gastrointestinal worms, lungworms, and ectoparasites in livestock, with nanomolar IC₅₀ values against key parasitic species. As a derivative of avermectin, it exhibits prolonged efficacy due to its high lipophilicity and extended half-life, making it effective for sustained parasite control.

Chemical Structure

Doramectin

CAS#117704-25-3

Theoretical Analysis

MedKoo Cat#: 561486

Name: Doramectin

CAS#: 117704-25-3

Chemical Formula: C50H74O14

Exact Mass: 898.5079

Molecular Weight: 899.13

Elemental Analysis: C, 66.79; H, 8.30; O, 24.91

Price and Availability

Size	Price	Availability
1g	USD 250.00	2 Weeks
2g	USD 450.00	2 Weeks
5g	USD 850.00	2 Weeks

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Synonym

Doramectin; Dectomax; Doramectina; Doramectine; Doramectinum; UK-67994; UK 67994; UK67994; NSC-760342; NSC 760342; NSC760342

IUPAC/Chemical Name

(1'R,2S,4'S,5S,6R,8'R,10'E,12'R,13'S,14'E,20'R,21'R,24'S)-6-Cyclohexyl-21',24'-dihydroxy-12'-{[(2R,4S,5S,6S)-5-{[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy}-4-methoxy-6-methyloxan-2-yl]oxy}-5,11',13',22'-tetramethyl-5,6-dihydro-3',7',19'-trioxaspiro[pyran-2,6'-tetracyclo[15.6.1.14,8.020,24]pentacosane]-10',14',16',22'-tetraen-2'-one

InChi Key

QLFZZSKTJWDQOS-CYWJOYLHSA-N

InChi Code

InChI=1S/C50H74O14/c1-27-13-12-16-34-26-57-47-42(51)30(4)21-37(50(34,47)54)48(53)60-36-22-35(63-49(25-36)20-19-29(3)45(64-49)33-14-10-9-11-15-33)18-17-28(2)44(27)61-41-24-39(56-8)46(32(6)59-41)62-40-23-38(55-7)43(52)31(5)58-40/h12-13,16-17,19-21,27,29,31-33,35-47,51-52,54H,9-11,14-15,18,22-26H2,1-8H3/b13-12+,28-17+,34-16+/t27-,29-,31-,32-,35+,36-,37-,38-,39-,40-,41-,42+,43-,44+,45-,46-,47+,49+,50+/m0/s1

SMILES Code

O=C(O[C@]1([H])C2)[C@]([C@]/34O)([H])C=C(C)[C@@H](O)[C@@]4([H])OCC3=C/C=C/[C@H](C)[C@@H](O[C@@H]5O[C@@H](C)[C@H](O[C@@H]6O[C@@H](C)[C@H](O)[C@@H](OC)C6)[C@@H](OC)C5)/C(C)=C/C[C@@](C1)([H])O[C@]72C=C[C@H](C)[C@@H](C8CCCCC8)O7

Appearance

Solid powder

Purity

>97% (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

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Doramectin is a derivative of Ivermectin (HY-15310). Doramectin is a potent antiparasitic antibiotic.

In vitro activity:

Western blot analysis demonstrated that DRM (doramectin) induced the accumulation of LC3I/LC3II and Atg5 in U87 and C6 cells when the DRM concentration was 15 µM. In addition, DRM (15 µM) induced degradation of p62 in U87 and C6 cells (Fig. 2D-G). In combination, these data suggested that DRM could promote autophagy initiation in GBM cells. Reference: Int J Oncol. 2022 Mar;60(3):29. https://pubmed.ncbi.nlm.nih.gov/35137919/

In vivo activity:

Doramectin (10 mg/kg) and clofazimine (400 mg/kg) were found to be active in vivo with worm burden reductions of 60.1% and 82.7%, respectively. Reference: PLoS Negl Trop Dis. 2015 Jul 31;9(7):e0003962. https://pubmed.ncbi.nlm.nih.gov/26230921/

	Solvent	mg/mL	mM
Solubility
	DMSO	75.0	83.41
	Ethanol	100.0	111.22

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 899.13 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. Chen C, Liang H, Qin R, Li X, Wang L, Du S, Chen Z, Meng X, Lv Z, Wang Q, Meng J, Gao A. Doramectin inhibits glioblastoma cell survival via regulation of autophagy in vitro and in vivo. Int J Oncol. 2022 Mar;60(3):29. doi: 10.3892/ijo.2022.5319. Epub 2022 Feb 9. PMID: 35137919; PMCID: PMC8857930. 2. Anchordoquy JM, Anchordoquy JP, Nikoloff N, Gambaro R, Padula G, Seoane A, Furnus C. Doramectin induced cytotoxic and genotoxic effects on bovine peripheral lymphocytes and cumulus cells in vitro. J Environ Sci Health B. 2019;54(2):147-154. doi: 10.1080/03601234.2018.1559569. Epub 2019 Jan 22. PMID: 30668218. 3. Panic G, Vargas M, Scandale I, Keiser J. Activity Profile of an FDA-Approved Compound Library against Schistosoma mansoni. PLoS Negl Trop Dis. 2015 Jul 31;9(7):e0003962. doi: 10.1371/journal.pntd.0003962. PMID: 26230921; PMCID: PMC4521867. 4. Davey RB, Pound JM, Klavons JA, Lohmeyer KH, Freeman JM, Olafson PU. Analysis of doramectin in the serum of repeatedly treated pastured cattle used to predict the probability of cattle fever ticks (Acari: Ixodidae) feeding to repletion. Exp Appl Acarol. 2012 Apr;56(4):365-74. doi: 10.1007/s10493-012-9525-1. Epub 2012 Feb 19. PMID: 22349982.

In vitro protocol:

In vivo protocol:

1. Panic G, Vargas M, Scandale I, Keiser J. Activity Profile of an FDA-Approved Compound Library against Schistosoma mansoni. PLoS Negl Trop Dis. 2015 Jul 31;9(7):e0003962. doi: 10.1371/journal.pntd.0003962. PMID: 26230921; PMCID: PMC4521867. 2. Davey RB, Pound JM, Klavons JA, Lohmeyer KH, Freeman JM, Olafson PU. Analysis of doramectin in the serum of repeatedly treated pastured cattle used to predict the probability of cattle fever ticks (Acari: Ixodidae) feeding to repletion. Exp Appl Acarol. 2012 Apr;56(4):365-74. doi: 10.1007/s10493-012-9525-1. Epub 2012 Feb 19. PMID: 22349982.

1: Zhu Y, Liang M, Yu J, Zhang B, Zhu G, Huang Y, He Z, Yuan J. Repurposing of Doramectin as a New Anti-Zika Virus Agent. Viruses. 2023 Apr 27;15(5):1068. doi: 10.3390/v15051068. PMID: 37243154; PMCID: PMC10221537. 2: Doramectin--a novel avermectin. Vet Parasitol. 1993 Jul;49(1):1-119. PMID: 8236732. 3: Cantón G, Urtizbiría F, Lloberas MM, Morrell E, Lanusse C, Lifschitz A. Iatrogenic doramectin overdosing causes toxicity in sheep: A case report. Vet Parasitol Reg Stud Reports. 2022 May;30:100722. doi: 10.1016/j.vprsr.2022.100722. Epub 2022 Mar 24. PMID: 35431078. 4: Cordero AM, Quek S, Mueller RS. Doramectin in the treatment of generalized demodicosis. Vet Dermatol. 2018 Apr;29(2):104-e41. doi: 10.1111/vde.12515. Epub 2017 Dec 29. PMID: 29285807. 5: Dang F, Xu Q, Qin Z, Xia H. Rationally Improving Doramectin Production in Industrial Streptomyces avermitilis Strains. Bioengineering (Basel). 2023 Jun 20;10(6):739. doi: 10.3390/bioengineering10060739. PMID: 37370670; PMCID: PMC10295569. 6: Tang M, Hu X, Wang Y, Yao X, Zhang W, Yu C, Cheng F, Li J, Fang Q. Ivermectin, a potential anticancer drug derived from an antiparasitic drug. Pharmacol Res. 2021 Jan;163:105207. doi: 10.1016/j.phrs.2020.105207. Epub 2020 Sep 21. PMID: 32971268; PMCID: PMC7505114. 7: Lye G, Jacob A, Pomroy W, Stafford K, Singh P. Pharmacokinetics of subcutaneously administered doramectin in alpacas. J Vet Pharmacol Ther. 2020 Mar;43(2):123-128. doi: 10.1111/jvp.12821. Epub 2019 Oct 29. PMID: 31660626. 8: Goudie AC, Evans NA, Gration KA, Bishop BF, Gibson SP, Holdom KS, Kaye B, Wicks SR, Lewis D, Weatherley AJ, et al. Doramectin--a potent novel endectocide. Vet Parasitol. 1993 Jul;49(1):5-15. doi: 10.1016/0304-4017(93)90218-c. PMID: 8236738. 9: Chen C, Liang H, Qin R, Li X, Wang L, Du S, Chen Z, Meng X, Lv Z, Wang Q, Meng J, Gao A. Doramectin inhibits glioblastoma cell survival via regulation of autophagy in vitro and in vivo. Int J Oncol. 2022 Mar;60(3):29. doi: 10.3892/ijo.2022.5319. Epub 2022 Feb 9. PMID: 35137919; PMCID: PMC8857930. 10: Larroza M, Soler P, Robles C, Cabrera R, Ballent M, Lanusse C, Lifschitz A. Doramectin efficacy against Psoroptes ovis in sheep: Evaluation of pharmacological strategies. Exp Parasitol. 2020 Nov;218:107998. doi: 10.1016/j.exppara.2020.107998. Epub 2020 Sep 15. PMID: 32941889. 11: Du S, Liang H, Zhou L, Chen C, Sun R, Zhang J, Meng X, Gao A. Effect of doramectin on programmed cell death pathway in glioma cells. Clin Transl Oncol. 2023 Oct;25(10):2871-2883. doi: 10.1007/s12094-023-03147-z. Epub 2023 Apr 21. PMID: 37084153. 12: Nentwig A, Oevermann A, Burgener IA. Doramectin-Intoxikation bei drei Katzenwelpen [Doramectin intoxication in 3 kittens]. Schweiz Arch Tierheilkd. 2014 Apr;156(4):179-83. German. doi: 10.1024/0036-7281/a000573. PMID: 24686818. 13: Sarre C, Claerebout E, Vercruysse J, Levecke B, Geldhof P, Pardon B, Alvinerie M, Sutra JF, Geurden T. Doramectin resistance in Haemonchus contortus on an alpaca farm in Belgium. Vet Parasitol. 2012 Apr 30;185(2-4):346-51. doi: 10.1016/j.vetpar.2011.10.003. Epub 2011 Oct 13. PMID: 22035850. 14: Jackson AE. In this issue - June 2019: Charles Sturt application process reviewed · Single-drench doramectin in Bos indicus-cross beef calves · No evidence for endemic heartworm in South Australia · Anaphylaxis associated with intravenous Alfaxan in a dog · Acute hypoventilation following Brunfelsia sp. Poisoning in a dog. Aust Vet J. 2019 Jun;97(6):171-172. doi: 10.1111/avj.12835. PMID: 31136693. 15: El-Saber Batiha G, Alqahtani A, Ilesanmi OB, Saati AA, El-Mleeh A, Hetta HF, Magdy Beshbishy A. Avermectin Derivatives, Pharmacokinetics, Therapeutic and Toxic Dosages, Mechanism of Action, and Their Biological Effects. Pharmaceuticals (Basel). 2020 Aug 17;13(8):196. doi: 10.3390/ph13080196. PMID: 32824399; PMCID: PMC7464486. 16: Conde MH, Borges DGL, Freitas MG, da Silva MC, Borges FA. First report of Dermatobia hominis resistant to doramectin in cattle. Vet Parasitol. 2021 Jan;289:109335. doi: 10.1016/j.vetpar.2020.109335. Epub 2020 Dec 11. PMID: 33373969. 17: Pardo C, Caplan JP, McKnight CA. Bugging Out: Human Doramectin Misuse in a Case of Delusional Parasitosis. J Acad Consult Liaison Psychiatry. 2021 Sep- Oct;62(5):551-552. doi: 10.1016/j.jaclp.2021.04.007. Epub 2021 May 5. PMID: 34083160. 18: Holsback L, Luppi PA, Silva CS, Negrão GK, Conde G, Gabriel HV, Balestrieri JV, Tomazella L. Anthelmintic efficiency of doramectin, fenbendazole, and nitroxynil, in combination or individually, in sheep worm control. Rev Bras Parasitol Vet. 2016 Jul-Sep;25(3):353-8. doi: 10.1590/S1984-29612016025. Epub 2016 Apr 12. PMID: 27096532. 19: Li JS, Wang JD, Yang LY, Zhang J, Zhang H, Wang XJ, Xiang WS. New doramectin analogs from mutant Streptomyces avermitilis NEAU1069-3. J Antibiot (Tokyo). 2014 Feb;67(2):187-9. doi: 10.1038/ja.2013.97. Epub 2013 Oct 9. PMID: 24105609. 20: Borgsteede FH, Dercksen DD, Huijbers R. Doramectin and albendazole resistance in sheep in The Netherlands. Vet Parasitol. 2007 Mar 15;144(1-2):180-3. doi: 10.1016/j.vetpar.2006.09.031. Epub 2006 Nov 17. PMID: 17113232.