(2R)-6-铵基-2-[(N-苯甲酰基甘氨酰)氨基]己酸酯

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: (2R)-6-铵基-2-[(N-苯甲酰基甘氨酰)氨基]己酸酯
• 中文别名: 马尿酰赖氨酸
• 英文名称: N^α-hippuryllysine
• 英文别名: hippuryl-lysine；6-azaniumyl-2-[(2-benzamidoacetyl)amino]hexanoate
• 化学式: C₁₅H₂₁N₃O₄
• 分子量: 307.349
• InChiKey: LRCZLURYHGISRZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2
• 重原子数：
  22
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  122
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  D-葡萄糖 、 (2R)-6-铵基-2-[(N-苯甲酰基甘氨酰)氨基]己酸酯 以 甲醇 为溶剂， 反应 4.0h， 以22.1 mg的产率得到Nε-(1-deoxy-D-fructos-1-yl)hippuryl-lysine
  参考文献：
  名称：

  Nε-（1-脱氧-D-果糖-1-基）马尿酰基赖氨酸的制备和表征。

  摘要：

  DOI：

  10.1016/0008-6215(92)80027-x

文献信息

• Use of 13C Labeling and NMR Spectroscopy for the Investigation of Degradation Pathways of Amadori Compounds
  作者：Kazuki Akira、Takao Hashimoto

  DOI：10.1248/bpb.28.344

  日期：——

  The degradation pathways of Amadori compounds in vivo have not been fully understood because of the lack of suitable techniques although the compounds are considered to be key intermediates in glycation, which contributes to the development of pathologies associated with various chronic and age-related diseases. A new approach using 13C labeling and NMR spectroscopy has thus been described to obtain more insight into the degradation pathways. A 13C-labeled model Amadori compound, [1-13C]Nε-(1-deoxy-D-fructos-1-yl)hippuryl-lysine, was synthesized to investigate the degradation pathways of the sugar moiety. The labeled compound was then incubated under aerobic and physiologic conditions, followed by analysis using 13C-NMR spectroscopy to obtain the degradation profile. Consequently, after 28-d incubation at least nine 13C signals due to 13C-labeled products were observed with those due to unlabeled hippuryl-lysine. These labeled products included not only carboxymethylated hippuryl-lysine as the major product and α- and β-glucose but also acetate and formate. These experiments demonstrate the potential of using a 13C label and NMR spectroscopy in that the technique provides the comprehensive profiling of the degradation products containing the labeled position in spite of their chemical structures.

  虽然阿莫多利化合物被认为是糖化过程中的关键中间体，而糖化是导致与各种慢性和老年相关疾病有关的病理发展的原因之一，但由于缺乏合适的技术，人们尚未完全了解阿莫多利化合物在体内的降解途径。因此，我们介绍了一种使用 13C 标记和核磁共振光谱的新方法，以便更深入地了解降解途径。为了研究糖分子的降解途径，我们合成了一种 13C 标记的模型 Amadori 化合物，即 [1-13C]Nε-(1-脱氧-<小>D-果糖-1-基)海马基赖氨酸。然后将标记的化合物在有氧和生理条件下进行培养，再利用 13C-NMR 光谱分析获得降解曲线。结果发现，经过 28 天的培养后，至少观察到 9 个 13C 信号，这些信号来自 13C 标记的产物和未标记的马尿酰赖氨酸。这些标记产物不仅包括主要产物羧甲基化的海泡石赖氨酸、α-和β-葡萄糖，还包括乙酸盐和甲酸盐。这些实验证明了使用 13C 标记和核磁共振光谱技术的潜力，因为该技术可以全面分析含有标记位置的降解产物，而无需考虑其化学结构。
• Method of preparation of stabilized thrombin-activatable fibrinolysis inhibitor (TAFI) and methods of use thereof
  申请人：——

  公开号：US20020177560A1

  公开（公告）日：2002-11-28

  The invention is directed in part to a purified form of stabilized activated thrombin-activatable fibrinolysis inhibitor (TAFIa). The invention is further directed to a method of producing stabilized TAFIa. The invention is also directed to methods for therapeutic use of stabilized TAFIa such as in the treatment, prevention or management of diseases via an anti-coagulant effect. The invention is also directed to methods for therapeutic use of inhibitors of TAFIa such as in the treatment, prevention or management of diseases via a procoagulant effect. The invention is also directed to methods of diagnostic use of stabilized TAFIa such as a standard in a chromogenic or a fluorometric carboxypeptidase activity assay. The present invention is also directed to kits comprising stabilized TAFIa useful in measuring carboxypepetidase activity.

  本发明部分涉及一种纯化形式的稳定活化凝血酶可激活纤溶抑制剂（TAFIa）。本发明进一步涉及生产稳定化 TAFIa 的方法。本发明还涉及稳定TAFIa的治疗使用方法，例如通过抗凝作用治疗、预防或控制疾病。本发明还涉及 TAFIa 抑制剂的治疗使用方法，例如通过促凝血作用治疗、预防或控制疾病。本发明还涉及稳定的 TAFIa 的诊断使用方法，如在显色或荧光羧肽酶活性测定中用作标准品。本发明还涉及用于测量羧肽酶活性的试剂盒，其中包含稳定的 TAFIa。
• Carboxypeptidases B from anopheles gambiae. compositions comprising them, vaccine applications and use as therapeutical targets
  申请人：Lavazec Catherine

  公开号：US20050260219A1

  公开（公告）日：2005-11-24

  The present invention provides two carboxypeptidase B enzymes from Anopheles gambiae and homologs thereof. The present invention also provides compositions and vaccines containing the carboxypeptidase B enzymes, as well as antibodies directed thereto and various methods of using the same. The methods of the present invention include a method of blocking Plasmodium development and a method of identifying compounds that inhibit carboxypeptidase B activity.

  本发明提供了两种羧肽酶 B 酶，它们来自 冈比亚按蚊 及其同源物。本发明还提供了含有羧肽酶 B 酶的组合物和疫苗，以及针对它们的抗体和使用它们的各种方法。本发明的方法包括阻断 疟原虫 发展的方法和鉴定抑制羧肽酶 B 活性的化合物的方法。
• Brinkmann, Elisabeth; Wells-Knecht, Kevin J.; Thorpe, Suzanne R., Journal of the Chemical Society. Perkin transactions I, 1995, # 22, p. 2817 - 2818
  作者：Brinkmann, Elisabeth、Wells-Knecht, Kevin J.、Thorpe, Suzanne R.、Baynes, John W.

  DOI：——

  日期：——
• Characterization of an Imidazolium Salt Formed from Glyoxal and N.alpha.-Hippuryllysine: A Model for Maillard Reaction Crosslinks in Proteins
  作者：Kevin J. Wells-Knecht、Elisabeth Brinkmann、John W. Baynes

  DOI：10.1021/jo00125a001

  日期：1995.10