DSM705 

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound^[1].

IC50: 95 nM (P. falciparum DHODH), 52 nM (P. vivax DHODH)^[1]

DSM705 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC₅₀=95 nM), P. vivax DHODH (PvDHODH, IC₅₀=52 nM) and Pf3D7 cells (EC₅₀=12 nM), with no inhibition of the human enzyme^[1].

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

DSM705 (3-200 mg/kg; p.o. twice a day for 6 days) provides the maximum rate of parasite killing at the dose of 50 mg/kg and fully suppresses parasitemia by days 7-8^[1].
DSM705 (2.6 and 24 mg/kg; a single p.o.) exhibits high oral bioavailability (74%, 70%), apparent t_1/2 (3.4, 4.5 h) and C_max (2.6, 20 μM) in Swiss outbred mice^[1].
DSM705 (2.3 mg/kg; a single i.v.) exhibits plasma clearance (CL=2.8 mL/min/kg) and V_ss (1.3 L/kg) in mice^[1].

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

404.39

C₁₉H₁₉F₃N₆O

2653225-38-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136.  [Content Brief]