1383846-83-0
中文名称
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-
英文名称
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
分子式
C30H25FN4O
分子量
476.54
MOL 文件
1383846-83-0.mol
结构式
基本信息
中文别名
化合物 T26705
英文别名
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-
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-
物理化学性质
| 沸点 | 732.5±70.0 °C(Predicted) |
| 密度 | 1.21±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 3.72±0.40(Predicted) |
应用领域
用途一
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.
常见问题列表
概述
AZ-4217 是 β 位淀粉样蛋白前体裂解酶 1 (BACE1) 的抑制剂，在人类 SH-SY5Y 细胞中的 IC50 为 160 pM。AZ-4217 可减少 Tg2576 小鼠模型中的淀粉样蛋白沉积，并用于阿尔茨海默病研究。