DSM705 hydrochloride，一种具有口服活性的抗疟化合物，是基于吡咯的二氢乳清酸脱氢酶 (DHODH) 抑制剂。DSM705 hydrochloride 对 Plasmodium DHODH 和 Plasmodium 寄生虫表现出纳摩尔级效力 (抑制 P. falciparum 和 P. vivax DHODH 的 IC₅₀ 分别为 95 nM 和 52 nM)，对哺乳动物 DHODH 没有抑制作用。

DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC 50 =95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs.

Solid

IC50: 95 nM (P. falciparum DHODH), 52 nM (P. vivax DHODH)

DSM705 hydrochloride shows inhibitory activity against P. falciparum DHODH ( Pf DHODH, IC50=95 nM), P. vivax DHODH ( Pv DHODH, IC50=52 nM) and Pf 3D7 cells (EC50=12 nM), with no inhibition of the human enzyme. 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) hydrochloride provides the maximum rate of parasite killing at the dose of 50 mg/kg and fully suppresses parasitemia by days 7-8.
DSM705 (2.6 and 24 mg/kg; a single p.o.) hydrochloride 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.
DSM705 (2.3 mg/kg; a single i.v.) hydrochloride exhibits plasma clearance (CL=2.8 mL/min/kg) and V ss (1.3 L/kg) in mice. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 100 mg/mL (226.83 mM; Need ultrasonic)配制储备液