| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Oxyclozanide targets the mitochondria of parasitic trematodes by acting as a proton ionophore. It uncouples oxidative phosphorylation, disrupting the proton gradient across the inner mitochondrial membrane. This leads to the dissipation of energy as heat and the inhibition of ATP synthesis, ultimately causing the death of the parasite. The compound is a salicylanilide derivative.
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| ln Vitro |
SARS-CoV-2 is inhibited by oxclozamide. strains of pseudointermedius having a MIC between 0.5 and 1 μg/mL[3]. SARS-CoV-2 is inhibited by oxclozamide. strains of pseudointermedius with a MIC range of 0.5-2 μg/mL [3]. Methicillin's minimum inhibitory concentration (MIC) for Staphylococcus aureus (MRSA) is 1 μg/mL [3].
Oxyclozanide is effective against Fasciola hepatica and other trematodes. As a proton ionophore, it uncouples oxidative phosphorylation in the target organism. The compound's anthelmintic activity has been demonstrated in vitro against liver flukes. |
| ln Vivo |
In both sheep and cattle, oxclozamide (15 mg/kg for sheep and 10 mg/kg for cattle; oral) has demonstrated antiparasitic efficacy [1]. Large doses of oxclozamide (1500–5000 mg/kg; oral, once)
In vivo, oxyclozanide is used in veterinary medicine for the treatment of fascioliasis in ruminants. It is effective against both adult and juvenile stages of Fasciola hepatica. The compound is administered orally, and its efficacy has been demonstrated in field studies. |
| Enzyme Assay |
In vitro assays for oxyclozanide involve measuring its effects on mitochondrial function in parasites. Isolated mitochondria from Fasciola hepatica are incubated with oxyclozanide, and oxygen consumption is measured using an oxygen electrode. The uncoupling of oxidative phosphorylation is assessed by measuring the dissipation of the proton gradient and the inhibition of ATP synthesis.
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| Cell Assay |
Cellular assays for oxyclozanide are performed using parasite cultures. Fasciola hepatica or other trematodes are cultured in vitro and treated with oxyclozanide at varying concentrations. Parasite viability is assessed by motility scoring or by measuring ATP levels. The minimum effective concentration is determined.
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| Animal Protocol |
Animal/Disease Models: Healthy male and female Wistar rats (100-150 g) [2] Doses: 5000, 3690, 2730, 2025 and 1500 mg/ kg
Route of Administration: oral administration; 5000, 3690, 2730, 2025 and 1500 mg/kg; primary Experimental Results: poisoning symptoms such as mental depression, rough hair, loss of appetite, cyanosis of lips, limbs, and tail. The high-dose group caused splenomegaly, liver bleeding spots, and stomach distension. In vivo animal studies with oxyclozanide are conducted in ruminants naturally or experimentally infected with Fasciola hepatica. Oxyclozanide is administered orally at the recommended dose. Efficacy is assessed by measuring the reduction in fecal egg counts or by counting the number of flukes in the liver at necropsy. |
| ADME/Pharmacokinetics |
Oxyclozanide is administered orally and is absorbed from the gastrointestinal tract. Its molecular weight is 401 g/mol. The compound is metabolized in the liver and excreted in bile and feces. Its half-life in ruminants supports single-dose treatment.
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| Toxicity/Toxicokinetics |
Oxyclozanide is generally well tolerated in ruminants at therapeutic doses. No significant adverse effects have been reported. The compound has a wide safety margin. It should not be used in animals with known hypersensitivity. Milk and meat withdrawal periods should be observed.
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| References |
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| Additional Infomation |
An anthelmintic used to treat liver fluke and tapeworm infections in grazing animals.
Oxyclozanide is a veterinary anthelmintic used for the treatment of fascioliasis in ruminants. It is a salicylanilide derivative that acts as a proton ionophore. The compound is available as an oral drench or in feed formulations. It is not approved for use in humans and is intended for veterinary use only. |
| Molecular Formula |
C13H6CL5NO3
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|---|---|
| Molecular Weight |
401.44
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| Exact Mass |
398.879
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| CAS # |
2277-92-1
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| PubChem CID |
16779
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
446.0±45.0 °C at 760 mmHg
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| Melting Point |
205 - 210ºC
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| Flash Point |
223.5±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.722
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| LogP |
8.67
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
415
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JYWIYHUXVMAGLG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H6Cl5NO3/c14-4-1-6(16)11(20)8(2-4)19-13(22)9-10(18)5(15)3-7(17)12(9)21/h1-3,20-21H,(H,19,22)
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| Chemical Name |
2,3,5-trichloro-N-(3,5-dichloro-2-hydroxyphenyl)-6-hydroxybenzamide
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| Synonyms |
ICI 46683; Diplin; Oxyclozanide
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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 : ~100 mg/mL (~249.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.23 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 | 2.4910 mL | 12.4552 mL | 24.9103 mL | |
| 5 mM | 0.4982 mL | 2.4910 mL | 4.9821 mL | |
| 10 mM | 0.2491 mL | 1.2455 mL | 2.4910 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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