Derquantel
* Please be kindly noted products are not for therapeutic use. We do not sell to patients.
| Category | Enzyme inhibitors |
| Catalog number | BBF-04000 |
| CAS | 187865-22-1 |
| Molecular Weight | 479.61 |
| Molecular Formula | C28H37N3O4 |
| Purity | >98% by HPLC |
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Description
Derquantel is a semi-synthetic paraherquamide analogue prepared by removal of the 2-oxo group in a four-step sequence of N-protection. Derquantel is an effective nematicide, which can act as a nicotinic acetylcholine receptor antagonist agent, causing flaccid paralysis and nematode repellent.
Specification
| Synonyms | 2-Deoxoparaherquamide; 2-Deoxoparaherquamide A; 2-Desoxoparaherquamide A; PF 00520904; PNU 141962 |
| Storage | Store at -20°C |
| IUPAC Name | (1S,6R,7R,9S,11R)-6-hydroxy-4',4',6,10,10,13-hexamethylspiro[3,13-diazatetracyclo[5.5.2.01,9.03,7]tetradecane-11,8'-9,10-dihydro-[1,4]dioxepino[2,3-g]indole]-14-one |
| Canonical SMILES | CC1(C=COC2=C(O1)C=CC3=C2NCC34CC56CN7CCC(C7(CC5C4(C)C)C(=O)N6C)(C)O)C |
| InChI | InChI=1S/C28H37N3O4/c1-23(2)10-12-34-21-18(35-23)8-7-17-20(21)29-15-26(17)14-27-16-31-11-9-25(5,33)28(31,22(32)30(27)6)13-19(27)24(26,3)4/h7-8,10,12,19,29,33H,9,11,13-16H2,1-6H3/t19-,25+,26-,27+,28-/m0/s1 |
| InChI Key | DYVLXWPZFQQUIU-WGNDVSEMSA-N |
| Source | Semi-synthetic |
Properties
| Appearance | White Solid |
| Antibiotic Activity Spectrum | parasites |
| Density | 1.34 g/cm3 |
| Solubility | Soluble in ethanol, methanol, DMF, DMSO |
Reference Reading
1.Production benefits from pre- and post-lambing anthelmintic treatment of ewes on commercial farms in the southern North Island of New Zealand.
Miller CM1, Ganesh S, Garland CB, Leathwick DM. N Z Vet J. 2015 Jul;63(4):211-9. doi: 10.1080/00480169.2015.1007108. Epub 2015 May 15.
AIMS: To measure the magnitude and variability in production responses to anthelmintic treatments administered to adult ewes around lambing.
2.Clinical safety of rapid sequential administration of moxidectin injection and oral derquantel-abamectin as a quarantine treatment for introduced sheep.
Bartram DJ1, Noé L, Krautmann MJ, Lane S, Geurden T. Vet Rec. 2013 Apr 20;172(16):426. doi: 10.1136/vr.101442. Epub 2013 Mar 23.
3.Derquantel and abamectin: effects and interactions on isolated tissues of Ascaris suum.
Puttachary S1, Trailovic SM, Robertson AP, Thompson DP, Woods DJ, Martin RJ. Mol Biochem Parasitol. 2013 Apr;188(2):79-86. doi: 10.1016/j.molbiopara.2013.02.004. Epub 2013 Mar 21.
Startect(®) is a novel anthelmintic combination of derquantel and abamectin. It is hypothesized that derquantel and abamectin interact pharmacologically. We investigated the effects of derquantel, abamectin and their combination on somatic muscle nicotinic acetylcholine receptors and pharyngeal muscle glutamate gated chloride receptor channels of Ascaris suum. We used muscle-strips to test the effects of abamectin, derquantel, and abamectin+derquantel together on the contraction responses to different concentrations of acetylcholine. We found that abamectin reduced the response to acetylcholine, as did derquantel. In combination (abamectin+derquantel), inhibition of the higher acetylcholine concentration response was greater than the predicted additive effect. A two-micropipette current-clamp technique was used to study electrophysiological effects of the anthelmintics on: (1) acetylcholine responses in somatic muscle and; (2) on l-glutamate responses in pharyngeal preparations.
4.Expression of five acetylcholine receptor subunit genes in Brugia malayi adult worms.
Li BW1, Rush AC1, Weil GJ1. Int J Parasitol Drugs Drug Resist. 2015 Jun 23;5(3):100-9. doi: 10.1016/j.ijpddr.2015.04.003. eCollection 2015.
Acetylcholine receptors (AChRs) are required for body movement in parasitic nematodes and are targets of "classical" anthelmintic drugs such as levamisole and pyrantel and of newer drugs such as tribendimidine and derquantel. While neurotransmission explains the effects of these drugs on nematode movement, their effects on parasite reproduction are unexplained. The levamisole AChR type (L-AChRs) in Caenorhabditis elegans is comprised of five subunits: Cel-UNC-29, Cel-UNC-38, Cel-UNC-63, Cel-LEV-1 and Cel-LEV-8. The genome of the filarial parasite Brugia malayi contains nine AChRs subunits including orthologues of Cel-unc-29, Cel-unc-38, and Cel-unc-63. We performed in situ hybridization with RNA probes to localize the expression of five AChR genes (Bm1_35890-Bma-unc-29, Bm1_20330-Bma-unc-38, Bm1_38195-Bma-unc-63, Bm1_48815-Bma-acr-26 and Bm1_40515-Bma-acr-12) in B. malayi adult worms. Four of these genes had similar expression patterns with signals in body muscle, developing embryos, spermatogonia, uterine wall adjacent to stretched microfilariae, wall of V as deferens, and lateral cord.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
