Mefluleucine
Based on 9 publication(s) in Google Scholar
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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- Pureté: 98.0%
- CAS No.: 2095886-80-7
- Formule: C7H13F2NO2
- Masse moléculaire:181.18
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Mefluleucine
More- Nature. 2025 Feb;638(8049):172-181. [Abstract]
- Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X. [Abstract]
- Neuron. 2023 Oct 4;111(19):3028-3040.e6. [Abstract]
- J Neurosci. 2026 Feb 3:e0958252026. [Abstract]
- Mol Immunol. 2025 Nov 28:189:1-12. [Abstract]
- bioRxiv. 2025 Jul 21.
- biorxiv. 2024 May 27.
- McGill University. 2023 Jul 5.
- bioRxiv. 2023 Apr 24.
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IF
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WB
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RT-PCR
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IF
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Flow Cytometry
Activité biologique
mTORC1[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.
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Animal Model:Male Sprague-Dawley rats weighing 250-260 g[2].
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Dosage:40, 80, 160 mg/kg.
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Administration:PO, single dose (160 mg/kg) or daily for a total of 7 days (40, 80 mg/kg).
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Result:Produced antidepressant effects.
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Animal Model:Male Sprague–Dawley (SD) rats weighed 250-400 g[1].
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Dosage:1 mg/kg, 5 mg/kg (Pharmacokinetic Design).
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Administration:I.V at 1 mg/kg and PO at 5 mg/kg.
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Result:Essentially 100% orally bioavailable with an elimination half-life in plasma of ~ 3 h.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2095886-80-7
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Appearance Solid
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Masse moléculaire 181.18
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Formule C7H13F2NO2
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Color White to off-white
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SMILES
N[C@@H](CC(C)(C(F)F)C)C(O)=O
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Synonyms
NV-5138
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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Nature
2025 Feb;638(8049):172-181. PMID: 39743596
Mefluleucine purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8049):172-181. [Abstract]
Organoids from the control, patient, and MDLS groups were cultured for 70 days with or without NV-5138 (Mefluleucine: 50 μM) treatment, and then immunostained with the oRG cell markers HOPX and pS6.
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Cell Metab
Nicotinamide metabolism face-off between macrophages and fibroblasts manipulates the microenvironment in gastric cancer. [Abstract]2024 Jun 18:S1550-4131(24)00189-X. PMID: 38897198
Mefluleucine purchased from MedChemExpress. Usage Cited in: Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X. [Abstract]
Mouse CD8+ T cells were treated with MNAM and rescued by agonist including C16 PAF (1μM, 24h), pCS (125μM, 24h), NV-5138 (Mefluleucine: 100μM, 24h), ionomycin (1μM, 24h) and PMA (50nM, 24h). Flow cytometry detected the cytotoxicity (GZMB, TNF-α and IFN-γ) of T cells.
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Neuron
Excitatory neuron-specific suppression of the integrated stress response contributes to autism-related phenotypes in fragile X syndrome. [Abstract]2023 Oct 4;111(19):3028-3040.e6. PMID: 37473758 -
J Neurosci
A Time-Sensitive Plasticity Distinguishes the Rapid and Sustained Synaptic Actions of Ketamine from Its (2 R,6 R)-Hydroxynorketamine Metabolite. [Abstract]2026 Feb 3:e0958252026. PMID: 41633835 -
Mol Immunol
Catalpol enhances mTORC1/HIF-1α/PDHK1-mediated oxidative metabolism that leads to promote the differentiation of Treg cells in RA. [Abstract]2025 Nov 28:189:1-12. PMID: 41317620
Mefluleucine purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2025 Nov 28:189:1-12. [Abstract]
Western blotting was used to examine the effects of CAT on the phosphorylation levels of P70S6K and 4EBP1 and the protein expression levels of HIF-1α and PDHK1 following pretreatment with NV5138 (Mefluleucine: 150 μM; 24 h).
Mefluleucine purchased from MedChemExpress. Usage Cited in: Mol Immunol. 2025 Nov 28:189:1-12. [Abstract]
RT-qPCR was used to examine the effect of CAT on FOXP3 mRNA expression following pretreatment with NV5138 (Mefluleucine: 150 μM; 24 h).
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Mefluleucine purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 21.
Rosettes in control and SPG11 14-day-old cortical organoids, either untreated or treated with NV5138 (Mefluleucine: 100 μM), were stained with DAPI and immunostained with antibodies against phosphorylated S6.
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Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Sengupta S, et al. Discovery of NV-5138, the first selective Brain mTORC1 activator. Sci Rep. 2019 Mar 11;9(1):4107. [Content Brief]
[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. [Content Brief]
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 |
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| 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 |