| Identification | Back Directory | [Name]
2(1H)-Pyridinone, 5-[(1R)-3-aMino-4-fluoro-1-[3-[5-(1-propyn-1-yl)-3-pyridinyl]phenyl]-1H-isoindol-1-yl]-1-ethyl-3-Methyl- | [CAS]
1383846-83-0 | [Synonyms]
AZ-4217
(AZ4217)
5-[(1R)-3-amino-4-fluoro-1-[3-(5-prop-1-ynylpyridin-3-yl)phenyl]isoindol-1-yl]-1-ethyl-3-methylpyridin-2-one
2(1H)-Pyridinone, 5-[(1R)-3-aMino-4-fluoro-1-[3-[5-(1-propyn-1-yl)-3-pyridinyl]phenyl]-1H-isoindol-1-yl]-1-ethyl-3-Methyl- | [Molecular Formula]
C30H25FN4O | [MDL Number]
MFCD25976956 | [MOL File]
1383846-83-0.mol | [Molecular Weight]
476.54 |
| Hazard Information | Back Directory | [Description]
AZ-4217 is a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice. AZ-4217 has IC50 160 pM in human SH-SY5Y cells with an excellent in vivo efficacy. AZ-4217 may have potential for treatment of AD. BACE1 inhibition thus addresses a key mechanism in AD and its potential as a therapeutic target is currently being addressed in clinical studies. | [Uses]
AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research[1]. | [References]
[1] Eketj?ll S, et al., AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice. J Neurosci. 2013 Jun 12;33(24):10075-84. DOI:10.1523/JNEUROSCI.1165-13.2013 |
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