2. PI3K/Akt/mTOR
  3. mTOR
  4. NV-5138 hydrochloride

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

CAS No. : 2639392-70-2

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5 mg USD 365 In-stock
10 mg USD 585 In-stock
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Based on 5 publication(s) in Google Scholar

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NV-5138 hydrochloride Related Antibodies

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  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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.
Clinical Trial
Molecular Weight

217.64

Formula

C7H14ClF2NO2
CAS No.
Appearance

Solid

Color

Off-white to brown

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1148.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.5947 mL 22.9737 mL 45.9474 mL 114.8686 mL
5 mM 0.9189 mL 4.5947 mL 9.1895 mL 22.9737 mL
10 mM 0.4595 mL 2.2974 mL 4.5947 mL 11.4869 mL
15 mM 0.3063 mL 1.5316 mL 3.0632 mL 7.6579 mL
20 mM 0.2297 mL 1.1487 mL 2.2974 mL 5.7434 mL
25 mM 0.1838 mL 0.9189 mL 1.8379 mL 4.5947 mL
30 mM 0.1532 mL 0.7658 mL 1.5316 mL 3.8290 mL
40 mM 0.1149 mL 0.5743 mL 1.1487 mL 2.8717 mL
50 mM 0.0919 mL 0.4595 mL 0.9189 mL 2.2974 mL
60 mM 0.0766 mL 0.3829 mL 0.7658 mL 1.9145 mL
80 mM 0.0574 mL 0.2872 mL 0.5743 mL 1.4359 mL
100 mM 0.0459 mL 0.2297 mL 0.4595 mL 1.1487 mL
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NV-5138 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NV-51382639392-70-2NV5138NV 5138mTORMammalian target of RapamycindepressionneurosciencemTORCBDNFsestrinlong-lastingInhibitorinhibitorinhibit

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