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| Targets |
Diclazuril targets apicomplexan parasites by inhibiting their development. Its mechanism is linked to the actin depolymerizing factor (ADF), a key protein in the parasite's actin dynamics. It has also shown binding affinity to the human pregnane X receptor (PXR).
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| ln Vitro |
Diclazuril exhibits excellent in vitro activity. It inhibits tachyzoite production of Toxoplasma gondii by >97% at 0.005 µg/mL. It inhibits merozoite production of Sarcocystis neurona by >80% at 0.1 ng/mL. Against Eimeria tenella, it has an IC₅₀ of 0.0008 ppm. It inhibits actin polymerization and depolymerization kinetics at 1 mg/L.
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| ln Vivo |
As a coccidiostat, diclazuril (R-64433) works. Strong, prolonged oocyst excretion was observed in lambs treated with diclazuril; the average level was 97.54 opg, substantially greater than those observed in animals treated with toltrazuril (p < 0.05)[1]. Late in the life cycle of Eimeria maxima, diclazuril (R-64433) is effective against it; nevertheless, subclinical intestinal abnormalities may appear soon after infection. Research has demonstrated that in birds with Eimeria major, diclazuril (R-64433) can lower lesion scores and enhance health and performance [2].
In vivo, diclazuril is highly effective. It reduces lesion scores and improves performance in broiler chickens challenged with Eimeria. In horses, it is used to treat EPM. In lambs treated with diclazuril, a persistent oocyst excretion was observed. |
| Enzyme Assay |
Diclazuril's binding affinity has been characterized using various assays. It shows competitive binding to human PXR with an EC₅₀ of 7.90 µM. It has also demonstrated strong binding to the DOP2 dopamine receptor in in silico studies. Its interaction with actin depolymerizing factor is studied via co-sedimentation analysis and TEM.
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| Cell Assay |
Diclazuril is highly active in cell culture. Treatment of T. gondii-infected cell cultures with 0.01 µg/mL for 3 days results in >99% reduction in tachyzoite counts. It inhibits merozoite production in bovine turbinate cell cultures infected with S. neurona.
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| Animal Protocol |
Diclazuril is extensively studied in animals. In poultry, it is administered in feed or water. In horses, it is given orally as a pelleted topdressing. Pharmacokinetic studies are performed in various species, including kiwi chicks and quails. Toxicological studies in zebrafish assess its developmental toxicity.
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| ADME/Pharmacokinetics |
In horses, plasma concentrations peak at 48 h (mean 395.6 ng/mL), while CSF peaks at 24 h (mean 9.0 ng/mL). The steady-state plasma concentration is 2000-2500 ng/mL. In lambs, absorption is poor, with Tmax at 24-48 h and a half-life of about 30 h. A physiologically based pharmacokinetic (PBPK) model has been developed for broiler chickens.
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| Toxicity/Toxicokinetics |
Diclazuril has a low order of toxicity. The NOEL in a two-year mouse study was 3 mg/kg bw/day. It has been shown to be safe in poultry without adverse effects. However, it has been detected in groundwater, raising concerns about its impact on non-target species.
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| References |
[1]. Diaferia, M., et al., Efficacy of toltrazuril 5 % suspension (Baycox(R), Bayer) and diclazuril (Vecoxan(R), Janssen-Cilag) in the control of Eimeria spp. in lambs. Parasitol Res, 2013. 112 Suppl 1: p. 163-8.
[2]. http://www.huvepharma.com/products/view/190 |
| Additional Infomation |
2-(4-Chlorophenyl)-2-[2,6-dichloro-4-(3,5-dioxo-1,2,4-triazin-2-yl)phenyl]acetonitrile is a nitrile compound. Diclazuril is an anticoccidial drug. See also: Banburmycin; Diclazuril (ingredient); Diclazuril; Virginiamycin (ingredient); Bacitracin methylene disalicylate; Diclazuril (ingredient).
Diclazuril is a triazine phenylacetonitrile anticoccidial agent. It is marketed under brand names such as Clinacox® for poultry and Protazil® for horses. It is not approved for human therapeutic use. Its primary research value lies in its use as a model anticoccidial for studying parasite biology and drug development. |
| Molecular Formula |
C17H9CL3N4O2
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|---|---|
| Molecular Weight |
407.63
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| Exact Mass |
405.979
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| CAS # |
101831-37-2
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| Related CAS # |
Diclazuril-d4;1632495-80-7
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| PubChem CID |
456389
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Melting Point |
548ºC
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| Index of Refraction |
1.702
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| LogP |
2.44
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
629
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C(C([H])=C(C=1C([H])(C#N)C1C([H])=C([H])C(=C([H])C=1[H])Cl)Cl)N1C(N([H])C(C([H])=N1)=O)=O
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| InChi Key |
ZSZFUDFOPOMEET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H9Cl3N4O2/c18-10-3-1-9(2-4-10)12(7-21)16-13(19)5-11(6-14(16)20)24-17(26)23-15(25)8-22-24/h1-6,8,12H,(H,23,25,26)
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| Chemical Name |
2-(4-chlorophenyl)-2-[2,6-dichloro-4-(3,5-dioxo-1,2,4-triazin-2-yl)phenyl]acetonitrile
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| Synonyms |
Diclazuril DCL Clinacox
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.33 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4532 mL | 12.2660 mL | 24.5321 mL | |
| 5 mM | 0.4906 mL | 2.4532 mL | 4.9064 mL | |
| 10 mM | 0.2453 mL | 1.2266 mL | 2.4532 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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