ELQ-300

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ELQ-300 是一种生物可利用的抗疟药，作为细胞色素 bc1 复合物 (cyt bc1) 还原 (Qi) 位点的抑制剂。

ELQ-300 is bioavailable antimalarial agent acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1).

ELQ-300 (0-70 nM, 21 d) inhibits P. falciparum Dd2, Tm90-C2B, and D1 growth with IC50 values of 6.6, 4.6 and 160 nM, respectively.

ELQ-300 (1 and 10 mg/kg; p.o. once daily for 1 or 4 days) inhibits P. yoelii growth in an acute infection model.ELQ-300 (10 and 20 mg/kg; p.o. once daily for 1 or 4 days) prevents recurrence of infection in mice. Animal Model:6-week female CF-1 mice with P. yoelii-WT infection Dosage:1 and 10 mg/kg Administration:Oral gavage; 1 mg/kg once daily for 4-day; 10 mg/kg once daily for 1-day Result:Inhibited P. yoelii with ED50 values of 0.04 and 0.03 mg/kg for 4-day dosing and 1-day dosing, respectively.Animal Model:6-week female CF-1 mice with P. yoelii-WT infection Dosage:10 and 20 mg/kg Administration:Oral gavage; 10 mg/kg once daily for 4-day; 20 mg/kg once daily for 1-day Result:Effectively prevented recrudescence in the 4-day dosing studies with infection mice.

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Microbiology/Virology

Parasite

Parasite

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1354745-52-0

475.85

C24H17ClF3NO4

>98% (HPLC)

DMSO:15.62 mg/mL?(32.83 mM)

COc1cc2[nH]c(C)c(-c3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3)c(=O)c2cc1Cl

6-Chloro-7-methoxy-2-methyl-3-{4-[4-(trifluoromethoxy)phenoxy]phenyl}quinolin-4(1H)-one

(-20℃)

With Ice Pack

≥ 2 years