NV-5138 是一种亮氨酸类似物，是首个具有选择性的、口服活性的脑内的 mTORC1 的激动剂，与 Sestrin2 结合。NV-5138 可用于抗抑郁的生物研究。
货号:ajcx35056
CAS:2095886-80-7
分子式:C7H13F2NO2
分子量：181.18
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1][2].

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[1].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[2].NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects[2].

[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.