DSM502, 恶性疟原虫二氢烟酸脱氢酶

DSM502

D656251-1ml

1ml

Moligand™

10mM in DMSO

-80℃储存

超低温冰袋运输

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice (23-36 g) were inoculated with parasites 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. IC50& Target:Plasmodium

DSM502 是一种基于吡咯的二氢烟酸脱氢酶 (DHODH) 抑制剂。DSM502 对疟原虫 DHODH 和疟原虫具有纳摩尔效力，对哺乳动物的 DHODH 没有抑制作用。

2426616-55-7(DMSO)

C16H16F3N3O

323.31 g/mol

O=C(C1=C(C)C(CC2=CC=C(C(F)(F)F)N=C2)=CN1)NC3CC3

恶性疟原虫二氢烟酸脱氢酶