DSM265 

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC₅₀ of 4.3 nM^[1][2].

IC50: 8.9 nM (PfDHODH)^[1]
EC50: 4.3 nM (P. falciparum 3D7 parasites)^[1]

DSM265 (0.5 to 75 mg/kg; Oral administration; twice daily; for 4 days; NOD-scid IL-2Rγnull (NSG) mice) has potent in vivo antimalarial activity with 90% effective dose (ED₉₀) 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) ^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

415.33

C₁₄H₁₂F₇N₅S

1282041-94-4

CC1=NC2=NC(C(C)(F)F)=NN2C(NC3=CC=C(S(F)(F)(F)(F)F)C=C3)=C1

Room temperature in continental US; may vary elsewhere.

• [1]. Kokkonda S, et al. Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparumDihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity. J Med Chem. 2016 Jun 9;59(11):5416-31.

  [2]. Phillips MA, et al. A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Sci Transl Med. 2015 Jul 15;7(296):296ra111.