DSM705 hydrochloride 是一种基于吡咯的二氢乳清酸脱氢酶 (DHODH) 抑制剂。DSM705 hydrochloride 对PlasmodiumDHODH 和Plasmodium寄生虫表现出纳摩尔级效力，对哺乳动物 DHODH 没有抑制作用。DSM705 hydrochloride 是一种有效的抗疟化合物。

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

DSM705 hydrochloride shows inhibitory activity against P. falciparum DHODH ( Pf DHODH, IC 50 =95 nM), P. vivax DHODH ( Pv DHODH, IC 50 =52 nM) and Pf 3D7 cells (EC 50 =12 nM), with no inhibition of the human enzyme [1].

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 [1]. 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 [1]. 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 [1]. Animal Model: SCID mice were inoculated with parasites [1] Dosage: 3, 10, 20, 50, 100, 200 mg/kg Administration: P.o. twice a day for 6 days Result: Killed parasite in a dose dependent manner and fully suppressed parasitemia by days 7-8. Animal Model: Swiss Outbred Mice [1] Dosage: 2.6 and 24 mg/kg for p.o.; 2.3 mg/kg for i.v. (Pharmacokinetic Analysis) Administration: A single p.o. and i.v. Result: P.o.: F=74/70%, t 1/2 =3.4/4.5 h, C max =2.6/20 μM. I.v.: CL=2.8 mL/min/kg, V ss =1.3 L/kg.

C19H20ClF3N6O

440.85

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years