| 产品描述: | RTI-7470-44 是一种有效且具有选择性和血脑屏障透过性的人微量胺相关受体 1 (hTAAR1) 拮抗剂,IC50 为 8.4 nM。
RTI-7470-44 具有中等的代谢稳定性和良好的初步脱靶谱。
RTI-7470-44 可增加小鼠中脑腹侧被盖区 (VTA) 多巴胺能神经元的自发放电率。
RTI-7470-44 可用于精神分裂症、活性分子成瘾和帕金森病 (PD) 的研究。 |
| 靶点: |
IC50: 8.4 nM (human TAAR1), 748 nM (rat TAAR1), 1190 nM (mouse TAAR1) |
| 体内研究: |
RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist). RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes. Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes. |
| 参考文献: |
1. Decker AM, et al. Identification of a Potent Human Trace Amine-Associated Receptor 1 Antagonist. ACS Chem Neurosci. 2022 Apr 6;13(7):1082-1095. |
| 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 |
2.223 ml |
11.115 ml |
22.23 ml |
| 5 mM |
0.445 ml |
2.223 ml |
4.446 ml |
| 10 mM |
0.222 ml |
1.112 ml |
2.223 ml |
| 50 mM |
0.044 ml |
0.222 ml |
0.445 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。 |