2. PI3K/Akt/mTOR
  3. mTOR
  4. Mefluleucine

Mefluleucine (NV-5138), a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. Mefluleucine is used for antidepressant studies.

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Mefluleucine

Mefluleucine Chemische Struktur

CAS. Nr. : 2095886-80-7

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Based on 9 publication(s) in Google Scholar

Other Forms of Mefluleucine:

Mefluleucine Related Antibodies

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mTOR mTORC1 mTORC2

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Beschreibung

Mefluleucine (NV-5138), a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. Mefluleucine is used for antidepressant studies[1][2].

IC50 & Target

mTORC1[1].
In Vivo

Mefluleucine (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].
Mefluleucine (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].
Mefluleucine (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.
Klinische Studie
Molekulargewicht

181.18

Formel

C7H13F2NO2
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](CC(C)(C(F)F)C)C(O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 10 mg/mL (55.19 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 5.5194 mL 27.5969 mL 55.1937 mL
5 mM 1.1039 mL 5.5194 mL 11.0387 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

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Volume (start)

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Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 98.0%

SDS (393 KB)

COA (250 KB) HNMR (244 KB) MS (177 KB)

Handling Instructions (2659 KB)
Verweise

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. 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 5.5194 mL 27.5969 mL 55.1937 mL 137.9843 mL
5 mM 1.1039 mL 5.5194 mL 11.0387 mL 27.5969 mL
10 mM 0.5519 mL 2.7597 mL 5.5194 mL 13.7984 mL
15 mM 0.3680 mL 1.8398 mL 3.6796 mL 9.1990 mL
20 mM 0.2760 mL 1.3798 mL 2.7597 mL 6.8992 mL
25 mM 0.2208 mL 1.1039 mL 2.2077 mL 5.5194 mL
30 mM 0.1840 mL 0.9199 mL 1.8398 mL 4.5995 mL
40 mM 0.1380 mL 0.6899 mL 1.3798 mL 3.4496 mL
50 mM 0.1104 mL 0.5519 mL 1.1039 mL 2.7597 mL
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  • 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:

Mefluleucine2095886-80-7NV-5138NV5138NV 5138mTORMammalian target of RapamycinInhibitorinhibitorinhibit

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