| 产品描述： | NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies |
| 靶点： |
mTORC1;mTOR |
| 体内研究： |
NV-5138 is found to be essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h determined following intravenous and oral dosing in rats. NV-5138 (160 mg/kg, po, single dose) rapidly increases levels of phospho-mTOR as well as the downstream targets, phospho-p70S6K1, and phosphor-4EB-P1, in synaptosomal preparations of PFC. NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects. Animal Model: Male Sprague-Dawley rats weighing 250-260 g. Dosage: 40, 80, 160 mg/kg. Administration: PO, single dose (160 mg/kg) or daily for a total of 7 days (40, 80 mg/kg). Result: Produced antidepressant effects. Animal Model: Male Sprague–Dawley (SD) rats weighed 250-400 g. Dosage: 1 mg/kg, 5 mg/kg (Pharmacokinetic Design). Administration: I.V at 1 mg/kg and PO at 5 mg/kg. Result: Essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h. |
| 参考文献： |
1. Sengupta S, et al. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. 2. Kato T, et al. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
5.519 ml |
27.596 ml |
55.193 ml |
| 5 mM |
1.104 ml |
5.519 ml |
11.039 ml |
| 10 mM |
0.552 ml |
2.76 ml |
5.519 ml |
| 50 mM |
0.11 ml |
0.552 ml |
1.104 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