Aliskiren(CGP 60536)是肾素抑制剂,IC50为1.5 nM。
阿利吉仑
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更新时间:2024-04-09 05:50:37
- 常用名阿利吉仑英文名aliskiren
- CAS号173334-57-1分子量551.758
- 密度1.1±0.1 g/cm3沸点748.4±60.0 °C at 760 mmHg
- 分子式C30H53N3O6熔点N/A
- MSDS闪点406.4±32.9 °C
- 符号信号词
阿利吉仑 名称
- 中文名阿利克仑
- 英文名aliskiren
- 中文别名阿利吉仑 |(2S,4S,5S,7S)-5-氨基-N-(2-氨基甲酰基-2-甲基丙基)-4-羟基-2-异丙基-7-[4-甲氧基-3-(3-甲氧基丙氧基)苄基]-8-甲基壬酰胺 |
- 英文别名(2S,4S,5S,7S)-7-(3-(3-Methoxypropoxy)-4-Methoxybenzyl)-5-aMino-N-(2-carbaMoyl-2-Methylpropyl)-4-hydroxy-2-isopropyl-8-MethylnonanaMide |Tekturna |(aS,S,dS,zS)-d-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)--hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide |Benzeneoctanamide, δ-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-γ-hydroxy-4-methoxy-3-(3-methoxypropoxy)-α,ζ-bis(1-methylethyl)-, (αS,γS,δS,ζS)- |Rasilez |(2S,4S,5S,7S)-5-Amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide |(2S,4S,5S,7S)-5-Amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methylnonanamide |Aliskiren |[14C]-Aliskiren |SPP 100 |(2S,4S,5S,7S)-7-(3-(3-Methoxypropoxy)-4-methoxybenzyl)-5-amino-N-(2-carbamoyl-2-methylpropyl)-4-hydroxy-2-isopropyl-8-methylnonanamide hydrochloride |
阿利吉仑 生物活性
- 描述Aliskiren(CGP 60536)是肾素抑制剂,IC50为1.5 nM。
- 相关类别信号通路 >> 自噬 >> 自噬 信号通路 >> 代谢酶/蛋白酶 >> 肾素 研究领域 >> 心血管疾病
- 参考文献[1]. Yuji Nakamura, et al. Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. ACS Med. Chem. Lett., 2012, 3 (9), pp 754–758 [2]. Buczko W, et al. Pharmacokinetics and pharmacodynamics of aliskiren, an oral direct renin inhibitor. Pharmacol Rep. 2008 Sep-Oct;60(5):623-31. [3]. Wood JM, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor.Biochem Biophys Res Commun, 2003, 308(4), 698-705. [4]. Gradman AH, et al.Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients. Circulation, 2005, 111(8), 1012-1018. [5]. Chang AY, et al. Interplay between brain stem angiotensins and monocyte chemoattractant protein-1 as a novel mechanism for pressor response after ischemic stroke. Neurobiol Dis. 2014 Nov;71:292-304.
阿利吉仑 物理化学性质
- 密度1.1±0.1 g/cm3
- 沸点748.4±60.0 °C at 760 mmHg
- 分子式C30H53N3O6
- 分子量551.758
- 闪点406.4±32.9 °C
- 精确质量551.393433
- PSA146.13000
- LogP2.74
- 蒸汽压0.0±2.6 mmHg at 25°C
- 折射率1.514
阿利吉仑 合成路线
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阿利吉仑 用途