产品
编 号：F754414
分子式：C19H19F3N6O
分子量：404.39
分子式：C19H19F3N6O
分子量：404.39
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CAS No: 2653225-38-6
产品详情
生物活性：
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.
体内研究：
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.DSM705 (2.6 and 24 mg/kg; a single p.o.) exhibits high oral bioavailability (74%, 70%), apparent t1/2 (3.4, 4.5 h) and Cmax (2.6, 20 μM) in Swiss outbred mice.DSM705 (2.3 mg/kg; a single i.v.) exhibits plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg) in mice.Animal Model:SCID mice were inoculated with parasites
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
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%, t1/2=3.4/4.5 h, Cmax=2.6/20 μM.I.v.: CL=2.8 mL/min/kg, Vss=1.3 L/kg.
体外研究：
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.
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.
体内研究：
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.DSM705 (2.6 and 24 mg/kg; a single p.o.) exhibits high oral bioavailability (74%, 70%), apparent t1/2 (3.4, 4.5 h) and Cmax (2.6, 20 μM) in Swiss outbred mice.DSM705 (2.3 mg/kg; a single i.v.) exhibits plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg) in mice.Animal Model:SCID mice were inoculated with parasites
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
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%, t1/2=3.4/4.5 h, Cmax=2.6/20 μM.I.v.: CL=2.8 mL/min/kg, Vss=1.3 L/kg.
体外研究：
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.
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