| 产品描述: | Vornorexant (ORN-0829; TS-142) 是一种有效的 OX1R 和 OX2R 双拮抗剂,IC50 值分别为 1.05 nM 和 1.27 nM。Vornorexant 在动物模型中表现出有效的睡眠促进作用,可作用于研究失眠。 |
| 靶点: |
OX2 Receptor |
| 体内研究: |
Vornorexant (oral administration; 1-10 mg/kg) exhibits potent sleep-promoting effects at a po. dose of 1 mg/kg in a rat polysomnogram study. It results in a dose-dependent increase in the percentage of total sleep. Vornorexant exhibits optimal PK properties with a rapid Tmax and short half-lives in rats and dogs. The T1/2 is 0.238 hours and 1.16 hours, respectively in rat and dog. |
| 参考文献: |
1. Aya Futamura, et al. Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia. Bioorg Med Chem. 2020 Jul 1;28(13):115489. |
| 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 |
2.235 ml |
11.174 ml |
22.348 ml |
| 5 mM |
0.447 ml |
2.235 ml |
4.47 ml |
| 10 mM |
0.223 ml |
1.117 ml |
2.235 ml |
| 50 mM |
0.045 ml |
0.223 ml |
0.447 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。 |