NV-5138 Datasheet | DC60095

NV-5138 — Datasheet

CAT. NO. DC60095

Parameter	Value
Chemical Name	4-(Difluoromethyl)-L-leucine
CAS No.	2095886-80-7
Synonyms	06CA9QMG6Z;4-(difluoromethyl)-L-leucine;N[C@H](C(=O)O)CC(C(F)F)(C)C;((S)-2-Amino-5,5-difluoro-4,4-dimethylpentanoic acid;Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-;K94
Formula	C7H13F2NO2
M.Wt	181.1804
SMILES	FC([H])(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[C@@]([H])(C(=O)O[H])N([H])[H])F
Purity	>98%
Storage	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 possesses rapid antidepressant effects[1][2].

In Vitro

No in vitro data are provided in the current product source. Contact us for further information.

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[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]. Animal Model: Male Sprague-Dawley rats weighing 250-260 g[2]. 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: Produces antidepressant effects. Animal Model: Male Sprague–Dawley (SD) rats weighed 250-400 g[1]. 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.

Target

mTORC1[1].

References & source

[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.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.