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| Other Sizes |
| Targets |
Nitroxynil targets the mitochondria of parasites. Its mechanism of action involves uncoupling oxidative phosphorylation in cellular mitochondria, which disturbs the production of ATP. This impairs parasite motility and leads to their death. As an anthelmintic, it is effective against liver flukes (Fasciola hepatica), gastrointestinal nematodes, and certain ectoparasites.
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| ln Vitro |
In vitro, Nitroxynil demonstrates potent anthelmintic activity. Its activity is assessed in assays measuring parasite motility or viability. The compound's ability to uncouple oxidative phosphorylation is confirmed by measuring ATP levels in treated parasites. It is effective against liver flukes and other parasites.
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| ln Vivo |
In vivo, Nitroxynil is effective at a dose of 10-20 mg/kg. It is primarily used in veterinary medicine to control liver flukes in livestock. It is administered via subcutaneous or intramuscular injection, as oral administration is less effective. It is also effective against gastrointestinal nematodes and certain ectoparasites.
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| Enzyme Assay |
For anthelmintic activity testing, Nitroxynil is evaluated in vitro against parasites such as Fasciola hepatica. Parasites are cultured and treated with varying concentrations of the compound. Parasite motility and viability are assessed microscopically, and the EC50 is determined. Its effect on mitochondrial function can be assessed by measuring ATP levels or oxygen consumption.
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| Cell Assay |
For cellular studies, parasite cells or mitochondrial preparations are used. The effect of Nitroxynil on mitochondrial function is assessed by measuring oxygen consumption or ATP production. The compound's ability to uncouple oxidative phosphorylation is confirmed by these assays.
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| Animal Protocol |
In vivo animal studies for Nitroxynil are conducted in livestock or laboratory animals infected with liver flukes or other parasites. The compound is administered via subcutaneous or intramuscular injection at a dose of 10-20 mg/kg. Efficacy is assessed by measuring parasite burden in the liver or other tissues. The compound's safety and efficacy are evaluated in these studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Nitroxynil are characterized in veterinary studies. It has a molecular weight of 290.015 and is almost insoluble in water. It is typically administered via injection. Its distribution, metabolism, and excretion have been studied in livestock.
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| Toxicity/Toxicokinetics |
Nitroxynil is a veterinary drug with a defined toxicity profile. It is effective at a dose of 10-20 mg/kg and is considered safe for use in livestock at recommended doses. However, it should be handled with caution, as it is a potent anthelmintic. It is intended for veterinary use only and is not for human therapeutic applications.
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| References |
[1]. Jiang R, et al. Cannabidiol is a potent inhibitor of the catalytic activity of cytochrome P450 2C19. Drug Metab Pharmacokinet. 2013;28(4):332-8.
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| Additional Infomation |
An anthelmintic intended for the treatment of liver fluke and liver clonorchiasis infections.
Nitroxynil is a potent anthelmintic agent with a molecular formula of C7H3IN2O3. It uncouples oxidative phosphorylation in parasite mitochondria, impairing ATP production and motility. It is used in veterinary medicine to control liver flukes and other parasites at a dose of 10-20 mg/kg. This veterinary compound is for research use only and has not been approved for human clinical applications. |
| Molecular Formula |
C7H3IN2O3
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|---|---|
| Molecular Weight |
290.01
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| Exact Mass |
289.918
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| CAS # |
1689-89-0
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| Related CAS # |
10532-59-9 (megulmate);1689-89-0;
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| PubChem CID |
15532
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| Appearance |
Off-white to light yellow solid powder
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| Density |
2.2±0.1 g/cm3
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| Boiling Point |
280.1±40.0 °C at 760 mmHg
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| Melting Point |
136 - 139ºC
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| Flash Point |
123.2±27.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.736
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| LogP |
2.8
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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 |
0
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| Heavy Atom Count |
13
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| Complexity |
256
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| Defined Atom Stereocenter Count |
0
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| SMILES |
IC1=C([H])C(C#N)=C([H])C(=C1O[H])[N+](=O)[O-]
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| InChi Key |
SGKGVABHDAQAJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H3IN2O3/c8-5-1-4(3-9)2-6(7(5)11)10(12)13/h1-2,11H
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| Chemical Name |
4-hydroxy-3-iodo-5-nitrobenzonitrile
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : 100 mg/mL (344.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.62 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 25.0 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 | 3.4482 mL | 17.2408 mL | 34.4816 mL | |
| 5 mM | 0.6896 mL | 3.4482 mL | 6.8963 mL | |
| 10 mM | 0.3448 mL | 1.7241 mL | 3.4482 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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