product name Clorsulon
Description: Clorsulon (also known as MK-401) is used in the treatment of Fasciola hepatica infections in calves and sheep. 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 (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.
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.
380.66
Formula
C8H8Cl3N3O4S2
CAS No.
60200-06-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 76 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 7 mg/mL (18.4 mM)
Solubility (In vivo)
1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
Synonyms
MK-401
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In 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. |
| Animal model | Rat |
| Formulation & Dosage | Formulated in 1:2 mixture of polyethylene glycol 400:dimethyl sulphoxide; 12.5 mg/kg; p.o. |
| 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. |
