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NV-5138

Chemical Structure : NV-5138

CAS No.: 2095886-80-7

NV-5138 (NV5138)

Catalog No.: PC-38176Not For Human Use, Lab Use Only.

NV-5138 (NV5138) is the first selective, orally bioavailable brain mTORC1 activator, binds to Sestrin2 (Kd=1.5 uM) and activates mTORC1 both in vitro and in vivo.

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Biological Activity

NV-5138 (NV5138) is the first selective, orally bioavailable brain mTORC1 activator, binds to Sestrin2 (Kd=1.5 uM) and activates mTORC1 both in vitro and in vivo.
NV-5138 activates mTORC1 by modulating the interaction between Sestrin2 and GATOR2 in cells.
NV-5138 is a selective small molecule that binds to Sestrin1/2 and differentiates from the natural ligand leucine by the lack of metabolism via the BCAT pathway and utilization in protein synthesis.
NV-5138 transiently activates mTORC1 in the brain in vivo.
A single dose of NV-5138 produced rapid and long-lasting antidepressant effects, and rapidly reversed anhedonia caused by chronic stress exposure.
NV-5138 also rapidly increased synapse number and function in the mPFC, and reversed the synaptic deficits caused by chronic stress in vivo.

Physicochemical Properties

M.Wt 181.183
Formula C7H13F2NO2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-2-amino-5,5-difluoro-4,4-dimethylpentanoic acid

References

1. Sengupta S, et al. Sci Rep. 2019 Mar 11;9(1):4107.

2. Kato T, et al. J Clin Invest. 2019 Apr 16;129(6):2542-2554. 

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