奥米沙班

• 常用名: 奥米沙班
• 英文名: Otamixaban
• CAS号: 193153-04-7
• 分子量: 446.498
• 密度: 1.3±0.1 g/cm3
• 沸点: N/A
• 分子式: C₂₅H₂₆N₄O₄
• 熔点: N/A
• 闪点: N/A

奥米沙班用途

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。

奥米沙班名称

• 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

奥米沙班生物活性

• 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.

奥米沙班物理化学性质

• 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
• InChIKey: PFGVNLZDWRZPJW-OPAMFIHVSA-N
• SMILES: COC(=O)C(Cc1cccc(C(=N)N)c1)C(C)NC(=O)c1ccc(-c2cc[n+]([O-])cc2)cc1
• 折射率: 1.619
• 储存条件: 2-8℃

奥米沙班靶点实验

查看更多实验

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：Selectivity ratio as Ki of Trypsin / Ki of factor Xa 来源：ChEMBL 靶标：N/A External Id：CHEMBL847407

实验名称：Selectivity ratio as Ki of Serine proteases tissue plasminogen activator / Ki of fact... 来源：ChEMBL 靶标：N/A External Id：CHEMBL847406

实验名称：Selectivity ratio as Ki of Plasmin / Ki of factor Xa 来源：ChEMBL 靶标：Coagulation factor X and plasma kallikrein External Id：CHEMBL847405

实验名称：Selectivity ratio as Ki of Activated protein C / Ki of factor Xa 来源：ChEMBL 靶标：N/A External Id：CHEMBL847404

实验名称：Selectivity ratio as Ki of factor IIA / Ki of factor Xa 来源：ChEMBL 靶标：Thrombin and coagulation factor X External Id：CHEMBL847408

实验名称：qHTS assay to identify novel small-molecules to repurpose for Merkel cell carcinoma t... 来源：NCGC 靶标：N/A External Id：MCC011

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奥米沙班英文别名

• 1ksn
• Otamixaban
• FXV-673
• Methyl (2R,3R)-2-(3-carbamimidoylbenzyl)-3-{[4-(1-oxido-4-pyridinyl)benzoyl]amino}butanoate
• UNII-S173RED00L