| 产品描述： | AF38469 is a new, specific and orally bioavailable Sortilin inhibitor (IC50: 330 nM). |
| 靶点： |
Neurotensin Receptor;NeurotensinReceptor |
| 体外研究： |
AF38469 showed no inhibition or stimulation of >50% at 10 μM in a standard selectivity panel of ca. 70 targets run at CEREP. Importantly AF38469 showed no activity against the NTR1 receptor. In addition, AF38469 showed no activity against a selected panel of targets known to bind acidic molecules (d-Opioid, GPR40, PPARd, EP1, Angiotensin AT1, Endothelin ETA & B, MMP-12). AF38469 will serve as an important tool to further delineate the biology of Sortilin, and to facilitate the evaluation of the therapeutic potential of this protein. |
| 体内研究： |
AF38469 (1 mg/kg；iv) 在大鼠中具有低分布容积 (血容量为 0.7 L/kg) 和低清除率 (4.8 L/h/kg)，半衰期 (t1/2) 为 1.2 h。 |
| 参考文献： |
1. Schroder TJ, et al. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin. Bioorg Med Chem Lett. 2014 Jan 1;24(1):177-80. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.084 ml |
15.42 ml |
30.84 ml |
| 5 mM |
0.617 ml |
3.084 ml |
6.168 ml |
| 10 mM |
0.308 ml |
1.542 ml |
3.084 ml |
| 50 mM |
0.062 ml |
0.308 ml |
0.617 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京