| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Clorsulon targets the metabolic pathways of liver flukes, particularly Fasciola hepatica and Fasciola gigantica. It is a competitive inhibitor of both 3-phosphoglycerate and ATP and inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro. By disrupting the energy metabolism of the parasite, Clorsulon leads to its death. The compound's specificity for fluke metabolic pathways makes it an effective anthelmintic agent with low toxicity to the host. Clorsulon is used in veterinary medicine, often in combination with other anthelmintics, for the treatment of fascioliasis in ruminants. Its mechanism of action is distinct from that of other flukicides, making it a valuable tool for parasite control.
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| ln Vitro |
Clorsulon is a competitive inhibitor of both 3-phosphoglycorate and ATP and had a Ki of 0.29 mM, inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro. Clorsulon is used in the treatment of Fasciola hepatica infections in calves and sheep. Target: Antiparasitic Clorsulon is a competitive inhibitor of both 3-phosphoglycorate and ATP and had a Ki of 0.29 mM, inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro.
In vitro studies have demonstrated that Clorsulon inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica. It acts as a competitive inhibitor of both 3-phosphoglycerate and ATP, disrupting the energy metabolism of the parasite. These in vitro findings provide a mechanistic basis for the compound's flukicidal activity. Clorsulon's activity against Fasciola hepatica and Fasciola gigantica has been confirmed in various in vitro assays using parasite cultures. The compound's potency and specificity for fluke metabolic pathways make it an effective anthelmintic agent. Further in vitro studies may explore its effects on different developmental stages of the parasite. |
| ln Vivo |
Clorsulon (a single dose of 15 mg/kg) is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). A 2.5 mg/kg dose removed over 90% of mature (16 weeks old) liver fluke from sheep. Clorsulon causes severe disruption to the tegument and gut of Fasciola hepatica after in vivo incubation.
In rats preliminarily infected with Fasciola hepatica metacercariae, a single oral dose of 3.1 mg/kg of Clorsulon (MK-401; L631529) eliminated more than 90% of flukes; the minimal effective level of the standard rafoxanide in the same test is also 3.1 mg/kg. [1] In sheep, a single oral dose of 15 mg/kg eliminated over 90% of F. hepatica that were 6 weeks of age (immature infection). [1] In sheep, a single oral dose of 2.5 mg/kg was 90% effective against mature (16 weeks old) F. hepatica infection. [1] In calves, a single oral dose of 15 mg/kg eliminated over 90% of F. hepatica that were 8 weeks of age. [1] In vivo studies have demonstrated that Clorsulon is effective in treating Fasciola hepatica infections in calves and sheep. A single oral dose of 15 mg/kg is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). The compound's efficacy against both immature and mature flukes makes it a valuable tool for the treatment of fascioliasis. Clorsulon is often used in combination with other anthelmintics to broaden the spectrum of activity against different parasites. The compound's favorable safety profile and efficacy have made it a widely used veterinary drug for the control of liver fluke infections in ruminants. |
| Enzyme Assay |
Non-cellular assays for Clorsulon typically involve measuring its effects on the metabolic enzymes of Fasciola hepatica. These assays use parasite extracts or purified enzymes to assess the inhibition of glucose utilization and acetate and propionate formation. Clorsulon is tested at various concentrations, and its inhibitory effects are measured by monitoring the production of metabolic products or the consumption of substrates. The compound's competitive inhibition of 3-phosphoglycerate and ATP can be assessed using enzyme kinetics assays. These assays provide a biochemical basis for the compound's flukicidal activity and help to elucidate its mechanism of action. Dose-response curves are generated, and IC50 values are calculated.
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| Cell Assay |
In vitro cell-based assays for Clorsulon are not typically performed, as the compound's activity is assessed against parasites rather than mammalian cells. However, cytotoxicity assays may be performed in mammalian cell lines to assess the compound's safety profile. These assays typically involve culturing cells in appropriate media and treating them with Clorsulon at various concentrations. Cell viability is assessed using MTT or similar assays. The compound's selectivity for parasite cells over mammalian cells is a key aspect of its safety profile. Clorsulon is typically dissolved in DMSO for in vitro studies. The compound's low toxicity to mammalian cells supports its use in veterinary medicine.
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| Animal Protocol |
Formulated in 1:2 mixture of polyethylene glycol 400:dimethyl sulphoxide; 12.5 mg/kg; p.o. Rat
In vivo animal studies for Clorsulon typically involve calves and sheep infected with Fasciola hepatica or Fasciola gigantica. Animals are treated with Clorsulon at various doses, typically administered orally as a single dose or as part of a combination therapy. The efficacy of the treatment is assessed by measuring the reduction in fluke burden at necropsy, as well as by monitoring clinical signs, weight gain, and hematological parameters. A single dose of 15 mg/kg is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). These studies are essential for establishing the optimal dosing regimen and efficacy of Clorsulon in veterinary practice. |
| ADME/Pharmacokinetics |
Pharmacokinetic studies of Clorsulon have shown that it is orally active and absorbed from the gastrointestinal tract. The compound is distributed to tissues, including the liver, where it reaches concentrations sufficient to kill liver flukes. Clorsulon is metabolized and excreted primarily in urine and feces. The compound's pharmacokinetic profile supports its use as a single oral dose for the treatment of fascioliasis. However, detailed PK parameters such as half-life, Cmax, AUC, and bioavailability are available in the veterinary pharmacology literature. Clorsulon is often used in combination with other anthelmintics to achieve broad-spectrum parasite control. The compound is approved for veterinary use in various countries.
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| Toxicity/Toxicokinetics |
In sheep, single oral doses of Clorsulon (MK-401; L631529) up to 400 mg/kg were tolerated without gross toxic symptoms. [1]
Toxicological data for Clorsulon indicate a favorable safety profile in calves and sheep at therapeutic doses. The compound is well-tolerated, with a wide margin of safety. However, specific toxicological studies, including acute and chronic toxicity, have been conducted as part of the drug development and regulatory approval process. Clorsulon is not intended for use in humans and is strictly a veterinary drug. The compound's safety profile in target animals has been established through extensive preclinical and clinical studies. As with all veterinary drugs, appropriate withdrawal periods should be observed before slaughter or milk production. |
| References |
J Med Chem.1977 Sep;20(9):1225-7;Mol Biochem Parasitol.1982 Mar;5(3):133-45;Parasitol Res.2004 Feb;92(3):232-41.
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| Additional Infomation |
4-Amino-6-(1,2,2-trichlorovinyl)benzene-1,3-disulfonamide is a sulfonamide belonging to the benzene family of compounds. See also: chlorsulfuron; ivermectin (one of the components).
Clorsulon (MK-401; L631529) is a fasciolicide active against both immature and mature Fasciola hepatica in sheep, calves, and rats. It was discovered through structural modification of 4-amino-6-(pentafluorothenyl)-1,3-benzenedisulfonamide. In rats, its efficacy (3.1 mg/kg) is comparable to that of rafoxanide. The compound is administered orally as a single dose. [1] Clorsulon (MK-401; L631529) is an orally active flukicidal agent used in veterinary medicine for the treatment of Fasciola hepatica and Fasciola gigantica infections in calves and sheep. It has the molecular formula C8H8Cl3N3O4S2 and CAS number 60200-06-8. Clorsulon inhibits glucose utilization and acetate and propionate formation by mature Fasciola hepatica. A single dose of 15 mg/kg removes over 90% of immature flukes from sheep and calves. Clorsulon is not approved for human use and is strictly a veterinary drug. |
| Molecular Formula |
C8H8CL3N3O4S2
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| Molecular Weight |
380.66
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| Exact Mass |
378.902
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| Elemental Analysis |
C, 25.24; H, 2.12; Cl, 27.94; N, 11.04; O, 16.81; S, 16.85
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| CAS # |
60200-06-8
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| Related CAS # |
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| PubChem CID |
43231
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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 |
651.7±65.0 °C at 760 mmHg
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| Melting Point |
194-203°C
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| Flash Point |
348.0±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.665
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| LogP |
1.04
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
604
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=C(/C(Cl)=C(Cl)\Cl)C=C(N)C(S(=O)(N)=O)=C1)(N)=O
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| InChi Key |
QOVTVIYTBRHADL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H8Cl3N3O4S2/c9-7(8(10)11)3-1-4(12)6(20(14,17)18)2-5(3)19(13,15)16/h1-2H,12H2,(H2,13,15,16)(H2,14,17,18)
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| Chemical Name |
4-Amino-6-(trichloroethenyl)-1,3-benzenedisulfonamide
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| Synonyms |
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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 |
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| 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 : 76~100 mg/mL ( 199.65~262.70 mM )
Ethanol : ~7 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 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 (6.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (6.57 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6270 mL | 13.1351 mL | 26.2702 mL | |
| 5 mM | 0.5254 mL | 2.6270 mL | 5.2540 mL | |
| 10 mM | 0.2627 mL | 1.3135 mL | 2.6270 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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