ELQ-300
目录号: PL08803 纯度: ≥98.0%
CAS No. :1354745-52-0
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中文名称
ELQ-300
英文名称
ELQ-300
英文别名
ELQ300;6-chloro-7-methoxy-2-methyl-3-[4-[4-(trifluoromethoxy)phenoxy]phenyl]-1H-quinolin-4-one;WZDNKHCQIZRDKW-UHFFFAOYSA-N;GTPL10021;BCP30856;ELQ300; ELQ 300;SB17071;Q15410945;6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1H)-one;6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy) phenyl) quinolin-4(1H)-one;6-Chloro-2-methyl-3-[4-[4-(trifluoromethoxy)phenoxy]phenyl]-7-methoxyquinol;ELQ-300
Cas No.
1354745-52-0
分子式
C24H17ClF3NO4
分子量
475.84
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ELQ-300 是一种有效的、有口服生物活性的抗疟疾剂,结合并抑制细胞色素 bc1 复合物 (cyt bc1) 的还原 (Qi) 位点。ELQ-300 抑制恶性疟原虫 Dd2,Tm90-C2B 和 D1 的 IC50 值分别为 6.6,4.6 和 160 nM。ELQ-300 可用于抗疟疾的研究。
生物活性
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Q i ) site of the cytochrome bc 1 complex (cyt bc 1 ). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC 50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial.
性状
Solid
IC50 & Target[1][2]
IC50: 6.6 nM (P. falciparum Dd2), 4.6 nM (P. falciparum Tm90-C2B), 160 nM (P. falciparum D1)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
[2]. Stickles AM, et al. Atovaquone and ELQ-300 Combination Therapy as a Novel Dual-Site Cytochrome bc1 Inhibition Strategy for Malaria. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4853-9.
溶解度数据
In Vitro: DMSO : 15.62 mg/mL (32.83 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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