NV-5138

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NV-5138 是一种选择性口服活性大脑 mTORC1 激活剂，具有抗抑郁作用。

NV-5138 is a selective and orally active activator of brain mTORC1, with antidepressant effects.

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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.

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PI3K/Akt/mTOR signaling

mTOR

mTORC1

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2095886-80-7

181.18

C7H13F2NO2

>98% (HPLC)

In Vitro:?DMSO : 10 mg/mL (55.19 mM)

O=C(O)[C@@H](N)CC(C)(C)C(F)F

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(-20℃)

With Ice Pack

≥ 2 years