| 产品描述: | AWZ1066S is a highly potent, specific and orally active anti-Wolbachia agent with EC50 value of 121 nM. AWZ1066S also is a weak CYP2C9 inhibitor and a weak CYP3A4 inducer with IC50 values of 9.7 μM and 37 uM, respectively. AWZ1066S can be used for the research of tropical diseases such as Onchocerciasis (river blindness) and lymphatic filariasis (elephantiasis) |
| 靶点: |
EC50: 121 nM (anti-Wolbachia);Parasite |
| 体外研究: |
AWZ1066S has anti-Wolbachia activity with EC50 value of 121 nM. AWZ1066S has a weak CYP2C9 inhibitory activity with an IC50 value of 9.7 μM and has a weak CYP3A4 induced activity with an IC50 value of 37 uM, but does not show any time-dependent inhibition across five majorhuman CYP450 isoforms (CYP1A, CYP2C9, CYP2C19, CYP2D6, CYP3A) |
| 体内研究: |
AWZ1066S (oral; 50, 100 mg/kg; bid; for 7 days) has high anti-Wolbachia efficacy. AWZ1066S (i.v or p.o; 5, 10, 85, 90 242 mg/kg) can oral delivery and has good aqueous solubility and metabolic stability |
| 参考文献: |
1. Hong WD, et al. AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.473 ml |
12.364 ml |
24.729 ml |
| 5 mM |
0.495 ml |
2.473 ml |
4.946 ml |
| 10 mM |
0.247 ml |
1.236 ml |
2.473 ml |
| 50 mM |
0.049 ml |
0.247 ml |
0.495 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。 |