DSM502 T40087

Product Introduction
Bioactivity


英文名: DSM502

描述: DSM502, a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor, demonstrates potent nanomolar activity against Plasmodium DHODH and Plasmodium parasites, while not inhibiting mammalian DHODHs.

体外活性: DSM502 shows inhibitory activity against P. falciparum DHODH ( Pf DHODH, IC 50 =20 nM), P. vivax DHODH ( Pv DHODH, IC 50 =14 nM) and Pf 3D7 cells (EC 50 =14 nM), with no inhibition of the human enzyme[1].

体内活性: DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study[1]. DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t 1/2 (2.6, 3.6 h) and C max (8.4, 42.3 μM) in mice[1]. DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t 1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and V ss (1.2 L/kg) in mice[1]. Animal Model: SCID mice (23-36 g) were inoculated with parasites[1]Dosage: 10 and 50 mg/kg Administration: P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites Result: Resulted in 97% parasite clearance compared to 85% clearance in the GSK study. The 10 mg/kg mouse died on day 5.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: DSM 502 | DSM502 | DSM-502

DSM502 T40087信息由TargetMol中国为您提供，如您想了解更多关于DSM502 T40087报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途