| Identification | Back Directory | [Name]
[4-[1-Hydroxy-3-methyl-1-(2-methylpropyl)butyl]-2H-1,2,3-triazol-2-yl]-1-pyrrolidinylmethanone | [CAS]
1361532-00-4 | [Synonyms]
AA74-1
AA74-1 >=98% (HPLC)
[4-(4-Hydroxy-2,6-dimethylheptan-4-yl)-2H-1,2,3-triazol-2-yl](pyrrolidin-1-yl)methanone
[4-[1-Hydroxy-3-methyl-1-(2-methylpropyl)butyl]-2H-1,2,3-triazol-2-yl]-1-pyrrolidinylmethanone
Methanone, [4-[1-hydroxy-3-methyl-1-(2-methylpropyl)butyl]-2H-1,2,3-triazol-2-yl]-1-pyrrolidinyl- | [Molecular Formula]
C16H28N4O2 | [MDL Number]
MFCD23704789 | [MOL File]
1361532-00-4.mol | [Molecular Weight]
308.42 |
| Chemical Properties | Back Directory | [Boiling point ]
454.1±37.0 °C(Predicted) | [density ]
1.18±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: >15mg/mL | [form ]
film | [pka]
13.03±0.29(Predicted) | [color ]
colorless |
| Hazard Information | Back Directory | [Uses]
AA74-1 is a potent and selective inhibitor of APEH. AA74-1 significantly increases T cells proliferation by blocking the APEH activity[1]. | [Biological Activity]
AA74-1 is an extremely potent and selective inhibitor of the serine hydrolase acyl-peptide hydrolase (APEH) with an IC50 of 5 nM in mouse T-cell proteomes. AA74-1 potently blocked the activity of its target serine hydrolaseAPEHin mice in vivo without significantly affecting other enzymes. The APEH inhibition caused accumulation of N-acetylated proteins and stimulated cellular proliferation in T cells.
The APEH gene is deleted in some cancersin which it has been proposed to serve as a potential tumor suppressorand is involved in the degradation of oligomeric amyloid-beta which could make it a new target for therapy aimed at reducing neurodegeneration in Alzheimerμs disease. AA74-1 is the first selective tool for studying APEH activity. | [References]
[1] Adibekian A, et al. Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors. Nat Chem Biol. 2011 May 15;7(7):469-78. DOI:10.1038/nchembio.579 |
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Energy Chemical
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CHEMSWORTH
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