NV-5138 | CAS#2095886-80-7

NV-5138
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555979

CAS#: 2095886-80-7

Description: NV-5138 is an orally and centrally active small-molecule drug for the treatment of major depressive disorder (MDD). It directly and selectively activates the mammalian target of rapamycin complex 1 (mTORC1) signaling pathway by binding to and modulating sestrin2, a leucine amino acid sensor and upstream regulatory pathway. The mTORC1 pathway is the same signaling pathway that the NMDA receptor antagonist ketamine activates in the medial prefrontal cortex (mPFC) to mediate its rapid-acting antidepressant effects. A single oral dose of NV-5138 has been found to increase mTORC1 signaling and produce synaptogenesis in the mPFC and to induce rapid antidepressant effects in multiple animal models of depression.

Chemical Structure

NV-5138

CAS# 2095886-80-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555979
Name: NV-5138
CAS#: 2095886-80-7
Chemical Formula: C7H13F2NO2
Exact Mass: 181.09
Molecular Weight: 181.183
Elemental Analysis: C, 46.40; H, 7.23; F, 20.97; N, 7.73; O, 17.66

Price and Availability

Size	Price	Availability
100mg	USD 1950	2 Weeks
200mg	USD 2950	2 Weeks
500mg	USD 3650	2 Weeks
1g	USD 4650	2 Weeks
2g	USD 7950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: NV-5138; NV 5138; NV5138;

IUPAC/Chemical Name: Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-

InChi Key: HRFIMCJTDKEPPV-BYPYZUCNSA-N

InChi Code: InChI=1S/C7H13F2NO2/c1-7(2,6(8)9)3-4(10)5(11)12/h4,6H,3,10H2,1-2H3,(H,11,12)/t4-/m0/s1

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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Product Data:

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Biological target:	NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2.
In vitro activity:	This study reports NV-5138, a novel orally bioavailable compound that binds to Sestrin2 and activates mTORC1 both in vitro and in vivo. Treatment with NV-5138 activates mTORC1 in leucine-starved unedited HEK-293T cells, but not in cells lacking all three Sestrins or the GATOR1 component Nprl3 indicating that compound activity requires an intact Sestrins/GATOR pathway (Fig. 2f,g). Reference: Sci Rep. 2019 Mar 11;9(1):4107. https://pubmed.ncbi.nlm.nih.gov/30858438/
In vivo activity:	The results demonstrate that a single dose of NV-5138 produced rapid and long-lasting antidepressant effects, and rapidly reversed anhedonia caused by chronic stress exposure. The antidepressant actions of NV-5138 required BDNF release as the behavioral responses are blocked by infusion of a BDNF neutralizing antibody into the medial prefrontal cortex (mPFC) or in mice with a knock-in of a BDNF polymorphism that blocks activity dependent BDNF release. NV-5138 administration also rapidly increased synapse number and function in the mPFC, and reversed the synaptic deficits caused by chronic stress. Reference: J Clin Invest. 2019 Apr 16;129(6):2542-2554. https://pubmed.ncbi.nlm.nih.gov/30990795/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	25.0	137.98

Preparing Stock Solutions

The following data is based on the product molecular weight 181.18 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Kato T, Pothula S, Liu RJ, Duman CH, Terwilliger R, Vlasuk GP, Saiah E, Hahm S, Duman RS. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. doi: 10.1172/JCI126859. PMID: 30990795; PMCID: PMC6546461. 2. Sengupta S, Giaime E, Narayan S, Hahm S, Howell J, O'Neill D, Vlasuk GP, Saiah E. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. doi: 10.1038/s41598-019-40693-5. PMID: 30858438; PMCID: PMC6412019.
In vitro protocol:	1. Sengupta S, Giaime E, Narayan S, Hahm S, Howell J, O'Neill D, Vlasuk GP, Saiah E. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. doi: 10.1038/s41598-019-40693-5. PMID: 30858438; PMCID: PMC6412019.
In vivo protocol:	1. Kato T, Pothula S, Liu RJ, Duman CH, Terwilliger R, Vlasuk GP, Saiah E, Hahm S, Duman RS. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. doi: 10.1172/JCI126859. PMID: 30990795; PMCID: PMC6546461. 2. Sengupta S, Giaime E, Narayan S, Hahm S, Howell J, O'Neill D, Vlasuk GP, Saiah E. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. doi: 10.1038/s41598-019-40693-5. PMID: 30858438; PMCID: PMC6412019.

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1: Hasegawa Y, Zhu X, Kamiya A. NV-5138 as a fast-acting antidepressant via direct activation of mTORC1 signaling. J Clin Invest. 2019 May 20;129(6):2207-2209. doi: 10.1172/JCI129702. PMID: 31107245; PMCID: PMC6546442.

2: Kato T, Pothula S, Liu RJ, Duman CH, Terwilliger R, Vlasuk GP, Saiah E, Hahm S, Duman RS. Sestrin modulator NV-5138 produces rapid antidepressant effects via direct mTORC1 activation. J Clin Invest. 2019 Apr 16;129(6):2542-2554. doi: 10.1172/JCI126859. PMID: 30990795; PMCID: PMC6546461.

3: Sengupta S, Giaime E, Narayan S, Hahm S, Howell J, O'Neill D, Vlasuk GP, Saiah E. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. doi: 10.1038/s41598-019-40693-5. PMID: 30858438; PMCID: PMC6412019.

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