Description
DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase ( Pf DHODH ) with an IC 50 of 8.9 nM. DSM265 can also inhibit the growth of Pf 3D7 parasites with an EC 50 of 4.3 nMIn VivoDSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD- scid IL-2Rγ (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose ( ED 90 ) of 3 mg/kg per day (1.5 mg/kg twice daily). The maximum rate of parasite killing occurred at and above a dose of 13 mg/kg per day (6.4 mg/kg twice daily). DSM265 has moderate terminal elimination half-life (t 1/2 ) of 2-4 hours for mice (0.5 to 75 mg/kg, oral). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD- scid IL-2Rγ (NSG) mice (23-36 g)Dosage: 0.5 to 75 mg/kg Administration: Oral administration; twice daily; for 4 days Result: Had potent antimalarial activity with 90% effective dose ( ED 90 ) of 3 mg/kg per day (1.5 mg/kg twice daily).Form:SolidIC50& Target:IC50: 8.9 nM ( Pf DHODH), EC50: 4.3 nM ( P. falciparum 3D7 parasites)