| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Letrazuril targets protozoal and bacterial pathogens through mechanisms that are not fully defined. As a triazinedione derivative structurally related to diclazuril, it is believed to interfere with mitochondrial function in susceptible organisms. The compound is effective against Cryptosporidium infections and shows inhibitory activity against Eimeria, Mycobacterium bovis BCG, and Mycobacterium tuberculosis. Its anti-HIV activity suggests additional mechanisms of action.
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| ln Vitro |
In vitro, letrazuril demonstrates inhibitory activity against Eimeria, Mycobacterium bovis BCG, and Mycobacterium tuberculosis. It is effective against Cryptosporidium infections. The compound also shows anti-HIV activity. Detailed IC₅₀ values for these activities are not extensively reported in the available literature. Its activity as an antiprotozoal agent is well-established through its use in veterinary medicine.
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| ln Vivo |
In vivo, letrazuril has been used in trials studying the treatment of HIV infection and cryptosporidiosis. It is an effective treatment for coccidiosis and has been used extensively in veterinary medicine. The compound's in vivo efficacy against Cryptosporidium infections has been demonstrated in clinical studies. Detailed in vivo data from animal models are not extensively reported in the available literature.
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| Enzyme Assay |
Non-cell-based assays for letrazuril are not typical, as its mechanism involves antiprotozoal and antibacterial activity. However, antimicrobial susceptibility testing can be performed using standard broth microdilution or agar dilution methods to determine minimum inhibitory concentrations (MICs) against susceptible organisms. For Mycobacterium tuberculosis, radiometric or colorimetric methods may be used.
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| Cell Assay |
Cellular assays for letrazuril are performed using cultures of susceptible organisms. For Cryptosporidium, cell culture systems using human intestinal epithelial cells can be used to assess inhibition of parasite growth. For Mycobacterium tuberculosis, macrophage infection models can be used to assess intracellular activity. The compound is added at various concentrations, and parasite or bacterial growth is measured using microscopy, metabolic assays, or colony counting.
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| Animal Protocol |
In vivo animal models for letrazuril include models of Cryptosporidium infection in immunocompromised animals (e.g., SCID mice) or neonatal animals. The compound is administered orally at various doses. Efficacy is assessed by measuring parasite burden in the intestines or by evaluating clinical signs of infection. For anti-HIV activity, relevant models would involve HIV-infected humanized mice or other appropriate systems.
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| ADME/Pharmacokinetics |
Letrazuril has a molecular weight of 391.18 g/mol and a molecular formula of C₁₇H₉Cl₂FN₄O₂. CAS number is 103337-74-2. The compound is soluble in DMSO at 50 mg/mL. Purity is ≥95%. Appearance is a solid powder. Storage conditions: powder at -20°C for 3 years; at 4°C for 2 years. The compound is supplied for research use only.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for letrazuril are not extensively reported in the available literature. As an antiprotozoal agent, its safety profile has been evaluated in clinical and veterinary settings. The compound is supplied for research use only and is not for human consumption in a research context. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Letrazuril has been used in trials investigating the treatment of HIV infection and cryptosporidiosis.
Letrazuril is a synthetic triazine derivative and the p-fluoro analog of diclazuril. It is an anti-HIV agent and an antiprotozoal agent effective against Cryptosporidium infections. The compound has inhibitory activity against Eimeria, Mycobacterium bovis BCG, and Mycobacterium tuberculosis. It has been used in trials studying the treatment of HIV infection and cryptosporidiosis. Letrazuril is used in research applications studying infectious diseases and antimicrobial therapy. It is for research use only. |
| Molecular Formula |
C17H9CL2FN4O2
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|---|---|
| Molecular Weight |
391.18
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| Exact Mass |
390.009
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| CAS # |
103337-74-2
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| PubChem CID |
59745
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| Appearance |
White to off-white solid powder
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| Density |
1.54g/cm3
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| Index of Refraction |
1.681
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| LogP |
3.434
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
632
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XQKYUBTUOHHNDV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H9Cl2FN4O2/c18-13-5-11(24-17(26)23-15(25)8-22-24)6-14(19)16(13)12(7-21)9-1-3-10(20)4-2-9/h1-6,8,12H,(H,23,25,26)
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| Chemical Name |
2-[2,6-dichloro-4-(3,5-dioxo-1,2,4-triazin-2-yl)phenyl]-2-(4-fluorophenyl)acetonitrile
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| Synonyms |
Letrazurilo; Letrazurilum; Letrazuril
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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 : ~50 mg/mL (~127.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.22 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (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 22.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5564 mL | 12.7818 mL | 25.5637 mL | |
| 5 mM | 0.5113 mL | 2.5564 mL | 5.1127 mL | |
| 10 mM | 0.2556 mL | 1.2782 mL | 2.5564 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.
Products are for research use only; We do not sell to patients
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