Clorsulon

Clorsulon (L631529; MK401) is an orally active flukicidal agent. Clorsulon inhibits glycolysis, the primary energy production pathway in flukes. Clorsulon is also a competitive inhibitor of 3-phosphoglycolate and ATP, inhibiting glucose utilization and acetate and propionate formation by mature Fasciola hepatica in vitro. Clorsulon can be used in studies of liver fluke (Fasciola hepatica and Fasciola gigantica) infection in calves and sheep^{[1][2][3][4][5][6]}. In Vitro:Clorsulon (10 μg/mL; 24 h) causes severe disruption to both tegument and gut of Fasciola hepatica when both absorption routes are available, with more severe damage to the gut^[3]. In Vivo:Clorsulon (12.5 mg/kg; p.o.) induces progressive ultrastructural damage to the tegument and gut of Fasciola hepatica in infected male Sprague-Dawley rats, with the gut more severely affected^[2].
Clorsulon (5 mg/kg; i.v.) is actively secreted into milk by Abcg2 in lactating wild-type mice, and co-administration with Ivermectin (HY-15310) reduces this secretion^[4].
Clorsulon (30-300 mg/kg/day; p.o.) induces reversible urothelial hyperplasia in male CrI:CD(SD) BR rats^[6].