Boc-D-Lys(Tfa)-NMeArg(Tos)-Gly-OSu | 167215-28-3

• 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
• 英文名称: Boc-D-Lys(Tfa)-NMeArg(Tos)-Gly-OSu
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 2-[[(2S)-5-[[amino-[(4-methylphenyl)sulfonylamino]methylidene]amino]-2-[methyl-[(2R)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-6-[(2,2,2-trifluoroacetyl)amino]hexanoyl]amino]pentanoyl]amino]acetate
• CAS: 167215-28-3
• 化学式: C₃₃H₄₇F₃N₈O₁₁S
• 分子量: 820.844
• InChiKey: OCBVZYAVILRHIY-PKTZIBPZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  56
• 可旋转键数：
  22
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.58
• 拓扑面积：
  273
• 氢给体数：
  5
• 氢受体数：
  15

反应信息

• 作为反应物：
  描述：

  Boc-D-Lys(Tfa)-NMeArg(Tos)-Gly-OSu 在 盐酸 、 N,N-二异丙基乙胺 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 生成 3-((4S,10S,13R)-13-amino-4-(2-(benzyloxy)-2-oxoethyl)-20,20,20-trifluoro-11-methyl-3,6,9,12,19-pentaoxo-10-(3-(3-tosylguanidino)propyl)-2,5,8,11,18-pentaazaicosyl)benzoic acid
  参考文献：
  名称：

  Tc-99m-labeled fibrinogen receptor antagonists: design and synthesis of cyclic RGD peptides for the detection of thrombi

  摘要：

  Tc-99m labeled derivatives of N-Me-Arg-Gly-Asp containing cyclic peptide GP IIb/IIIa receptor antagonists are potential radiopharmaceuticals for the diagnosis of thrombosis. The design and synthesis of these peptides are described. These compounds are incorporated in rapidly growing thrombi under both arterial and venous conditions in canine models. Thrombi are clearly visible in images acquired at 50 min. Copyright (C) 1996 The DuPont Merck Pharmaceutical Company.

  DOI：

  10.1016/0960-894x(96)00282-x
• 作为产物：
  描述：

  N-MeArg(Tos)-Gly-OBzl 在 palladium on activated charcoal 氢气 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 、 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 Boc-D-Lys(Tfa)-NMeArg(Tos)-Gly-OSu
  参考文献：
  名称：

  Tc-99m-labeled fibrinogen receptor antagonists: design and synthesis of cyclic RGD peptides for the detection of thrombi

  摘要：

  Tc-99m labeled derivatives of N-Me-Arg-Gly-Asp containing cyclic peptide GP IIb/IIIa receptor antagonists are potential radiopharmaceuticals for the diagnosis of thrombosis. The design and synthesis of these peptides are described. These compounds are incorporated in rapidly growing thrombi under both arterial and venous conditions in canine models. Thrombi are clearly visible in images acquired at 50 min. Copyright (C) 1996 The DuPont Merck Pharmaceutical Company.

  DOI：

  10.1016/0960-894x(96)00282-x

文献信息

• Radiolabeled platelet GPIIb/IIIa receptor antagonists as imaging agents
  申请人：The Dupont Merck Pharmaceutical Company

  公开号：US05879657A1

  公开（公告）日：1999-03-09

  This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.

  本发明提供了一种新型放射性药物，其为含有碳环或杂环环系统的放射性标记的环状化合物，可作为血小板糖蛋白IIb/IIIa复合物的拮抗剂；以及使用该放射性药物作为诊断动脉和静脉血栓的成像剂的方法；还提供了用于制备该放射性药物的新型试剂和包含该试剂的试剂盒。