| 产品描述： | FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations. |
| 靶点： |
human HDAC:3 nM (IC50);Plasmodium HDAC:31 nM (IC50);HDAC1:25 nM (IC50);HDAC2:29 nM (IC50);HDAC3:2 nM (IC50) |
| 体外研究： |
FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection. |
| 体内研究： |
FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite. |
| 参考文献： |
1. Potluri V, et al. Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J. 2020;19(1):365. Published 2020 Oct 12.
|
| 保存条件： |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.416 ml |
12.08 ml |
24.16 ml |
| 5 mM |
0.483 ml |
2.416 ml |
4.832 ml |
| 10 mM |
0.242 ml |
1.208 ml |
2.416 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.483 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