| 产品描述: | VU0469650 是一种有效的、选择性的、穿透 CNS 的 mGlu1 受体的反向变构调节剂,其 IC50 为99 nM。 |
| 靶点: |
mGluR 1:99 nM (IC50);GluR |
| 体内研究: |
VU0469650 (male Sprague-Dawley rats, 0.2 mg/kg, IV, once) exhibits moderate to high clearance, a moderate volume of distribution, and a half-life of approximately 1 hour. VU0469650 (male Sprague-Dawley rats, 10 mg/kg, IP, once) shows an excellent selectivity profile and good exposure in both plasma and brain samples. |
| 参考文献: |
1. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718. |
| 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 |
2.744 ml |
13.718 ml |
27.436 ml |
| 5 mM |
0.549 ml |
2.744 ml |
5.487 ml |
| 10 mM |
0.274 ml |
1.372 ml |
2.744 ml |
| 50 mM |
0.055 ml |
0.274 ml |
0.549 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。 |