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ELQ-300

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Chemical Structure| 1354745-52-0 同义名 : -
CAS号 : 1354745-52-0
货号 : A1177242
分子式 : C24H17ClF3NO4
纯度 : 98%+
分子量 : 475.844
MDL号 : MFCD28386233
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 15 mg/mL(31.52 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Stickles AM, et al. Subtle changes in endochin-like quinolone structure alter the site of inhibition within the cytochrome bc1 complex of Plasmodium falciparum. Antimicrob Agents Chemother. 2015 Apr;59(4):1977-82