Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-
- Product Name
- Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-
- CAS No.
- 2095886-80-7
- Chemical Name
- Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)-
- Synonyms
- NV-5138;NV-5138, 10 mM in DMSO;(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
- CBNumber
- CB75970354
- Molecular Formula
- C7H13F2NO2
- Formula Weight
- 181.18
- MOL File
- 2095886-80-7.mol
Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)- Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)- Chemical Properties,Usage,Production
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
Pentanoic acid, 2-amino-5,5-difluoro-4,4-dimethyl-, (2S)- Preparation Products And Raw materials
Raw materials
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