193153-04-7

• 常用中文名：奥米沙班
• 常用英文名：Otamixaban
• CAS号：193153-04-7
• 分子式：C₂₅H₂₆N₄O₄
• 分子量：446.498
• 相关类别： 信号通路 代谢酶/蛋白酶 因子Xa
• 发布时间：2018-03-06 08:00:00
• 更新时间：2026-07-03 20:25:02
• Otamixaban（FXV673）是高效的fXa选择性可逆型抑制剂，Ki为0.5nM，能抑制游离型或凝血酶原酶结合型fXa。

名称

• 中文名: 奥米沙班
• 英文名: methyl (2R,3R)-2-[(3-carbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate
• 中文别名: (2R,3R)-2-[3-脒基苄基]-3-[[4-(1-氧化-4-吡啶基)苯甲酰基]氨基]丁酸甲酯; 奥美沙班; (2R,3R)-2-(3-甲脒基-苄基)-3-[4-(1-氧基-吡啶-4-基)苯甲酰]氨基}-丁酸甲酯; 甲基(2R,3R)-2-{3-[氨基(亚胺基)甲基]苄基}-3-{[4-(1-氧化吡啶-4-YL)苯甲酰]氨基}戊酯
• 英文别名: Methyl (2R,3R)-2-[3-amidinobenzyl]-3-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]butanoate; 1ksn; FXV673/FXV-673; (αR)-3-(AMinoiMinoMethyl)-α-[(1R)-1-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]ethyl]benzenepropanoic Acid Methyl Ester; [R-(R*,R*)]-3-(AMinoiMinoMethyl)-α-[1-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]ethyl]benzenepropanoic Acid Methyl Ester; FXV-673; methyl (2R,3R)-2-[(3-cbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate; Methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[4-(1-oxido-4-pyridinyl)benzoyl]amino}butanoate; benzenepropanoic acid, 3-(aminoiminomethyl)-α-[(1R)-1-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]ethyl]-, methyl ester, (αR); Methyl (2R,3R)-2-{3-[amino(iMino)Methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate; UNII-S173RED00L; FXV 673; FXV673; FXV-673; Preluent; OtaMixaban

物化性质

• 密度: 1.3±0.1 g/cm3
• 分子式: C₂₅H₂₆N₄O₄
• 分子量: 446.498
• 精确质量: 446.195404
• PSA: 130.73000
• LogP: 0.58
• 折射率: 1.619
• 储存条件: 2-8℃

生物活性

• 描述: Otamixaban(FXV673)是高效的fXa选择性可逆型抑制剂,Ki为0.5nM,能抑制游离型或凝血酶原酶结合型fXa。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 因子Xa
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Eikelboom JW, Weitz JI.Otamixaban in acute coronary syndromes.Lancet. 2009 Sep 5;374(9692):762-4. Epub 2009 Aug 28.

  [2]. Sabatine MS, Antman EM, et al. Otamixaban for the treatment of patients with non-ST-elevation acute coronary syndromes (SEPIA-ACS1 TIMI 42): a randomised, double-blind, active-controlled, phase 2 trial.Lancet. 2009 Sep 5;374(9692):787-95. Epub 2009 Aug 28

  [3]. Guertin KR, Choi YM.The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development.Curr Med Chem. 2007;14(23):2471-81.

  [4]. Cohen M, Bhatt DL, et al. SEPIA-PCI Trial Investigators.Randomized, double-blind, dose-ranging study of otamixaban, a novel, parenteral, short-acting direct factor Xa inhibitor, in percutaneous coronary intervention: the SEPIA-PCI trial.Circulation. 2007

  [5]. Guertin, Kevin R.; Choi, Yong-Mi.The discovery of the factor Xa inhibitor Otamixaban: from lead identification to clinical development.Current Medicinal Chemistry (2007), 14(23), 2471-2481.