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  3. NV-5138 hydrochloride

NV-5138 hydrochloride 

Cat. No.: HY-114384B
Handling Instructions

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.

For research use only. We do not sell to patients.

NV-5138 hydrochloride Chemical Structure

NV-5138 hydrochloride Chemical Structure

Size Price Stock Quantity
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2050 In-stock
Estimated Time of Arrival: December 31
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100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target

mTORC1[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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: Produced 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.
Molecular Weight

217.64

Formula

C₇H₁₄ClF₂NO₂

SMILES

N[[email protected]@H](CC(C)(C(F)F)C)C(O)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1148.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5947 mL 22.9737 mL 45.9474 mL
5 mM 0.9189 mL 4.5947 mL 9.1895 mL
10 mM 0.4595 mL 2.2974 mL 4.5947 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (9.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (9.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (9.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NV-5138NV5138NV 5138mTORMammalian target of RapamycindepressionneurosciencemTORCBDNFsestrinlong-lastingInhibitorinhibitorinhibit

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Product Name:
NV-5138 hydrochloride
Cat. No.:
HY-114384B
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