NV-5138 hydrochloride, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 hydrochloride is used for antidepressant studies[2].IC50 & Target: mTORC1.In Vivo: 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[2].
NV-5138 (80 mg/kg, po, daily for a total of 7 days) also produces antidepressant effects[2].