| 产品描述: | CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy. |
| 靶点: |
PI4K:0.9 ± 0.1 nM (IC50);PI3Kδ:104 ± 3 nM (IC50);PI3Kα:191 ± 36 nM (IC50);PI3Kγ:324 ± 19 nM (IC50);PI3Kβ:392 ± 27 nM (IC50);Vps34:681 ± 25 nM (IC50) |
| 体外研究: |
CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase.
CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum. |
| 体内研究: |
CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model. |
| 参考文献: |
1. 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium. Eur J Med Chem. 2020 Feb 15;1 |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8°C,Inert atmosphere |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.482 ml |
12.412 ml |
24.823 ml |
| 5 mM |
0.496 ml |
2.482 ml |
4.965 ml |
| 10 mM |
0.248 ml |
1.241 ml |
2.482 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.496 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。 |