NV-5138 |
| カタログ番号GC63121 |
ロイシン類似体である NV-5138 は、セストリン 2 に結合する最初の選択的かつ経口的に活性な脳 mTORC1 アクチベーターです。
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Cas No.: 2095886-80-7
Sample solution is provided at 25 µL, 10mM.
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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.
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