| Size | Price | Stock | Qty |
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| 5g |
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| Other Sizes |
| Targets |
Antiprotozoal
Toltrazuril targets Coccidia parasites. It alters the fine structure of coccidial developmental stages, mostly through enlargement of the endoplasmic reticulum and Golgi apparatus, as well as anomalies in the perinuclear space and interference with nuclear division. It reduces the activity of oxidoreductases. |
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| ln Vitro |
Toltrazuril (BAY-i 9142) is an antiprotozoal drug that targets coccidioidal parasites. Toltrazuril alters the fine structure of coccidial developmental stages, mostly through enlargement of the endoplasmic reticulum and Golgi apparatus, as well as anomalies in the perinuclear space and interference with nuclear division. Toltrazuril therapy resulted in a considerably lower average opg compared to group C (5.78 opg vs. 144.62 opg) (p < 0.05), with 97.7% FOCR. A high efficacy rate (99.23%) was seen 15 days following therapy; nonetheless, the drug's average efficacy remained extremely high (>90%) across all studies.
In vitro, toltrazuril alters the fine structure of coccidian development stages, mainly due to a swelling of the endoplasmic reticulum and of the Golgi apparatus and to abnormalities in the peri-nuclear space, disturbance in nuclear division. Its antiprotozoal activity has been demonstrated in cell-based assays. |
| ln Vivo |
Sheep coccidiosis is a pathology caused by protozoan parasites of the genus Eimeria spp. with clinical and economic effect especially in young animals (Ambrosi 1995; Pellérdy 1974). A field study was conducted to evaluate the efficacy of a metaphylactic treatment with toltrazuril 5 % suspension (Baycox®, Bayer) in comparison with diclazuril (Vecoxan®, Janssen-Cilag) and untreated controls against naturally acquired Eimeria infections in housed lambs. A total of 170 animals, aged 24 to 34 days and randomly divided in three homogeneous groups, were included in the study. The assessment of treatment efficacy was based on total faecal oocyst excretion (opg) and count reduction (FOCR) in the two groups of animals treated with toltrazuril (TOLT) and diclazuril (DICL) compared with untreated control group (C). The animals treated with toltrazuril showed a considerably lower mean opg to that of group C (5.78 opg versus 144.62 opg) (p < 0.05) and a FOCR of 97.7 %. The higher efficacy (99.23 %) was observed at 15 days post treatment; however, the average efficacy of the drug remained extremely high (> 90 %) for all the study. The lambs treated with diclazuril showed an intense, persistent oocyst excretion with average levels of 97.54 opg, (p < 0.05). This study demonstrates the good efficacy of toltrazuril administered orally to lambs in the prepatent period in subclinical natural Eimeria infections in housed lambs[2].
In vivo, toltrazuril is used in veterinary medicine to treat coccidiosis caused by Eimeria species in poultry, livestock, and other animals. It is an antiprotozoal agent that acts upon Coccidia parasites. Its efficacy in treating coccidiosis has been demonstrated in various animal species. |
| Enzyme Assay |
The activity of toltrazuril can be assessed using cell-based assays with cultured Coccidia parasites. Parasites are incubated with varying concentrations of the compound, and cell viability is measured. The IC50 for antiprotozoal activity is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of toltrazuril, Coccidia parasites are treated with the compound, and the effects on parasite morphology, replication, and viability are assessed.
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| Animal Protocol |
In vivo studies with toltrazuril typically involve administration to animals via oral routes. In models of coccidiosis, the compound's effects on parasite clearance, disease progression, and animal health are assessed.
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| ADME/Pharmacokinetics |
Toltrazuril has a molecular formula of C18H14F3N3O4S and a molecular weight of 425.38. Its CAS number is 69004-03-1. The compound is an antiprotozoal agent. It is soluble in DMSO (85 mg/ml) and insoluble in water and ethanol. The purity is typically >98%.
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| Toxicity/Toxicokinetics |
Toltrazuril is generally well-tolerated in animals at therapeutic doses. Specific toxicity data are not detailed in the available literature. As with all veterinary drugs, it should be used according to label instructions.
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| References | |
| Additional Infomation |
1-Methyl-3-[3-methyl-4-[4-(trifluoromethylthio)phenoxy]phenyl]-1,3,5-triazine-2,4,6-trione is an aromatic ether.
Toltrazuril is a broad-spectrum anticoccidial agent used in veterinary medicine to treat coccidiosis. It acts upon Coccidia parasites and alters their fine structure. It is an important drug for the control of coccidiosis in poultry and livestock. |
| Molecular Formula |
C18H14F3N3O4S
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|---|---|
| Molecular Weight |
425.3817
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| Exact Mass |
425.065
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| Elemental Analysis |
C, 50.82; H, 3.32; F, 13.40; N, 9.88; O, 15.04; S, 7.54
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| CAS # |
69004-03-1
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| Related CAS # |
Toltrazuril (sulfone);69004-04-2
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| PubChem CID |
68591
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
194-196°C
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| Index of Refraction |
1.640
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
655
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC(=C1)N2C(=O)NC(=O)N(C2=O)C)OC3=CC=C(C=C3)SC(F)(F)F
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| InChi Key |
OCINXEZVIIVXFU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H14F3N3O4S/c1-10-9-11(24-16(26)22-15(25)23(2)17(24)27)3-8-14(10)28-12-4-6-13(7-5-12)29-18(19,20)21/h3-9H,1-2H3,(H,22,25,26)
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| Chemical Name |
1-methyl-3-[3-methyl-4-[4-(trifluoromethylsulfanyl)phenoxy]phenyl]-1,3,5-triazinane-2,4,6-trione
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| Synonyms |
Toltrazuril; 69004-03-1; Baycox; Toltrazurilo; Toltrazurilum; bay vi 9142; Bay-i 9142; Toltrazurilum [Latin];
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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 : ~130 mg/mL (~305.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (7.64 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 32.5 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 | 2.3508 mL | 11.7542 mL | 23.5084 mL | |
| 5 mM | 0.4702 mL | 2.3508 mL | 4.7017 mL | |
| 10 mM | 0.2351 mL | 1.1754 mL | 2.3508 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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