| 产品描述： | ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial |
| 靶点： |
IC50: 6.6 nM (P. falciparum Dd2), 4.6 nM (P. falciparum Tm90-C2B), 160 nM (P. falciparum D1) |
| 体内研究： |
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. |
| 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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.102 ml |
10.508 ml |
21.015 ml |
| 5 mM |
0.42 ml |
2.102 ml |
4.203 ml |
| 10 mM |
0.21 ml |
1.051 ml |
2.102 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.42 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京