Clorsulon is a competitive 8-phosphoglycerate kinase and phospho-glyceromutase inhibitor. Clorsulon is used as a potent internal and external parasites inhibitor. Clorsulon is an antihelminthic compound. Clorsulon is agent belonging to the benzenesulphonamide family which is recommended for the treatment and control of adult liver flukes in cattle as suspension for oral use or injectable formulations for subcutaneous administrations. Clorsulon inhibits the enzymes involved in the glycolytic pathway, the primary source of energy in flukes. Clorsulon also depresses ATP levels in the fluke. The acute toxicity of clorsulon is tested after oral and intraperitoneal administration in mice and rats. The oral LD50 value is higher than 10g/kg body weight in both species while those obtained after intraperitoneal administrations ranged between 678 to 938 mg/kg body weight.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Rat |
| Formulation | 1:2 mixture of polyethylene glycol 400:dimethyl sulphoxide |
| Dosages | 12.5 mg/kg |
| Administration | Orally |
| Molecular Weight | 380.66 |
| Formula | C8H8Cl3N3O4S2 |
| CAS Number | 60200-06-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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