848141-11-7

• 常用中文名：Alvelestat
• 常用英文名：Alvelestat
• CAS号：848141-11-7
• 分子式：C₂₅H₂₂F₃N₅O₄S
• 分子量：545.534
• 相关类别： 生物化工 抑制剂 蛋白酶体(Proteases) Serine Protease 抑制剂
• 发布时间：2017-10-18 02:49:36
• 更新时间：2024-01-13 20:31:07
• Alvelestat (AZD9668)是新型口服人neutrophil elastase（NE）抑制剂，pIC50和Ki分别为7.9和4.9 nM。

名称

• 中文名: Alvelestat
• 英文名: 6-methyl-1-(3-methylphenyl)-5-(2-methylpyrazol-3-yl)-N-[(5-methylsulfonylpyridin-2-yl)methyl]-2-oxopyridine-3-carboxamide
• 英文别名: Alvelestat [INN]; 3-Pyridinecarboxamide, 1,2-dihydro-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[[5-(methylsulfonyl)-2-pyridinyl]methyl]-2-oxo-1-[3-(trifluoromethyl)phenyl]-; Alvelestat; 6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-{[5-(methylsulfonyl)-2-pyridinyl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydro-3-pyridinecarboxamide; AZD9668; N-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide

物化性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 780.4±60.0 °C at 760 mmHg
• 分子式: C₂₅H₂₂F₃N₅O₄S
• 分子量: 545.534
• 闪点: 425.8±32.9 °C
• 精确质量: 545.134460
• PSA: 124.33000
• LogP: 0.50
• 蒸汽压: 0.0±2.7 mmHg at 25°C
• 折射率: 1.628
• 储存条件: -20°C

生物活性

• 描述: Alvelestat (AZD9668)是新型口服人neutrophil elastase(NE)抑制剂,pIC50和Ki分别为7.9和4.9 nM。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 弹性蛋白酶
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. Stevens T, et al. AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.

  [2]. Kuna P, et al. AZD9668, a neutrophil elastase inhibitor, plus ongoing budesonide/formoterol in patients with COPD. Respir Med. 2012 Apr;106(4):531-9.

  [3]. Vogelmeier C, et al. A randomised, placebo-controlled, dose-finding study of AZD9668, an oral inhibitor of neutrophil elastase, in patients with chronic obstructive pulmonary disease treated with tiotropium. COPD. 2012 Apr;9(2):111-20.

  [4]. Gunawardena KA, et al. Pharmacokinetics and safety of AZD9668, an oral neutrophil elastase inhibitor, in healthy volunteers and patients with COPD. Int J Clin Pharmacol Ther. 2013 Apr;51(4):288-304.