生物活性 | |||
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描述 | Complex III of the mitochondrial electron transport chain, also known as the cytochrome bc1 complex (cyt bc1), is a validated target for multistage antimalarial therapy. ELQ-300, a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of cyt bc1. ELQ-300 sensitized P. falciparum Dd2, Tm90-C2B, and D1 strains with IC50s of 6.6, 4.6 and 160 nM, respectively. Compared to the 6-halogen compounds ELQ-314, ELQ-296, and ELQ-339, ELQ-300 demonstrated both increased potency and more pronounced D1 cross-resistance, which correlated with halogen size[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.10mL 0.42mL 0.21mL |
10.51mL 2.10mL 1.05mL |
21.02mL 4.20mL 2.10mL |
参考文献 |
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