173334-57-1

• 常用中文名：阿利吉仑
• 常用英文名：Aliskiren
• CAS号：173334-57-1
• 分子式：C₃₀H₅₃N₃O₆
• 分子量：551.758
• 相关类别： 原料药 循环系统用药 抗高血压病药
• 发布时间：2018-04-17 08:00:00
• 更新时间：2024-01-02 18:31:54
• Aliskiren(CGP 60536)是肾素抑制剂,IC50为1.5 nM。

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

物化性质

• 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
• PSA: 146.13000
• LogP: 2.74
• 蒸汽压: 0.0±2.6 mmHg at 25°C
• 折射率: 1.514
• 储存条件: 2-8℃，干燥，密封

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.

安全

• 危害码 (欧洲): Xi

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