| Identification | Back Directory | [Name]
Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)- | [CAS]
2095886-80-7 | [Synonyms]
NV-5138
(2S)-2-amino-5,5-difluoro-4,4-dimethylpentanoic acid
Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-
inhibit,Inhibitor,NV-5138,mTOR,NV5138,Mammalian target of Rapamycin,NV 5138 | [Molecular Formula]
C7H13F2NO2 | [MDL Number]
MFCD32215303 | [MOL File]
2095886-80-7.mol | [Molecular Weight]
181.18 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C,unstable in solution, ready to use. | [solubility ]
DMSO: 10mM | [form ]
A solid | [color ]
White to off-white | [InChI]
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 | [InChIKey]
HRFIMCJTDKEPPV-BYPYZUCNSA-N | [SMILES]
C(O)(=O)[C@@H](N)CC(C)(C)C(F)F |
| Hazard Information | Back Directory | [Uses]
NV-5138, a leucine analog, is the first selective and orally active brain mTORC1 activator, binding to Sestrin2. NV-5138 is used for antidepressant studies[1][2]. | [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]. | 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. |
| [References]
[1] Sengupta S, et al. 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
[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. DOI:10.1172/JCI126859 |
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| Company Name: |
Twochem Co.Ltd
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| Telephone: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
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