5-acetamido-2-[2-[5-acetamido-6-hydroxy-2-(hydroxymethyl)-4-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-4-hydroxy-6-[(1R,2R)-1,2,3-trihydroxypropyl]oxane-2-carboxylic acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-acetamido-2-[2-[5-acetamido-6-hydroxy-2-(hydroxymethyl)-4-(3,4,5-trihydroxy-6-methyloxan-2-yl)oxyoxan-3-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-4-hydroxy-6-[(1R,2R)-1,2,3-trihydroxypropyl]oxane-2-carboxylic acid
• 化学式: C₃₁H₅₂N₂O₂₃
• 分子量: 820.7
• InChiKey: NIGUVXFURDGQKZ-TUNRMZNMSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -8.3
• 重原子数：
  56
• 可旋转键数：
  14
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.9
• 拓扑面积：
  403
• 氢给体数：
  15
• 氢受体数：
  23

文献信息

• LINKABLE LEWIS X ANALOGS
  申请人：Ranganathan Ramachandran

  公开号：US20110229409A1

  公开（公告）日：2011-09-22

  Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLe X ) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLe X compositions. In particular, the disclosed SLe X compounds can be used to prepare selectin binding ligand con-jugatcs by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLe X compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl Le X , and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

  本文披露了一类可连接四糖化合物，其中包括唾液酸Lewis X（SLeX）的氨基苯基糖苷和相关类似物。这些化合物具有可共轭的亲核基团，因此它们在制备多聚SLeX组分方面是有用的。特别地，所披露的SLeX化合物可用于通过将它们与报告物质（如对比剂、放射性诊断剂或细胞毒素或化疗剂）连接起来，制备选择素结合配体共轭物。本发明的SLeX化合物和共轭物表现出与天然唾液酸LeX相似的选择素结合性，因此可用于诊断和治疗选择素介导的疾病和相关病症。
• DETECTION OF HIGH RISK DRUSEN
  申请人：APELLIS PHARMACEUTICALS, INC.

  公开号：US20160067357A1

  公开（公告）日：2016-03-10

  In some aspects, methods of detecting complement activation in vivo, e.g., in an eye, are provided. In some aspects, methods of detecting high risk drusen are provided. In some aspects, presence of one or more high risk drusen in an eye indicates increased likelihood of developing AMD, GA, or advanced AMD or increased likelihood of rapid progression of AMD. In some embodiments, methods comprise detecting drusen containing or in close proximity to complement activation. In some embodiments methods comprise detecting one or more drusen having inflamed endothelium underlying or in close proximity thereto. In some embodiments methods comprise detecting eye-derived extracellular microvesicles, e.g., exosomes, in a body fluid. In some embodiments methods comprise detecting Th17 cells or a Th17 biomarker in a body fluid. In some embodiments the Th17 biomarker is a cytokine. Methods may be applied individually or in any combination. In some embodiments any of the methods further comprises treating a subject at risk of developing AMD, GA, or advanced AMD or at increased likelihood of rapid progression of AMD with a complement inhibitor. In some aspects, agents useful for performing one or more of the methods are described.
• US7422733B2
  申请人：——

  公开号：US7422733B2

  公开（公告）日：2008-09-09
• [EN] DETECTION OF HIGH RISK DRUSEN<br/>[FR] DÉTECTION DE DRUSEN À RISQUE ÉLEVÉ
  申请人：APELLIS PHARMACEUTICALS INC

  公开号：WO2014028861A1

  公开（公告）日：2014-02-20

  In some aspects, methods of detecting complement activation in vivo, e.g., in an eye, are provided. In some aspects, methods of detecting high risk drusen are provided. In some aspects, presence of one or more high risk drusen in an eye indicates increased likelihood of developing AMD, GA, or advanced AMD or increased likelihood of rapid progression of AMD. In some embodiments, methods comprise detecting drusen containing or in close proximity to complement activation. In some embodiments methods comprise detecting one or more drusen having inflamed endothelium underlying or in close proximity thereto. In some embodiments methods comprise detecting eye-derived extracellular microvesicles, e.g., exosomes, in a body fluid. In some embodiments methods comprise detecting Th17 cells or a Th17 biomarker in a body fluid. In some embodiments the Th17 biomarker is a cytokine. Methods may be applied individually or in any combination. In some embodiments any of the methods further comprises treating a subject at risk of developing AMD, GA, or advanced AMD or at increased likelihood of rapid progression of AMD with a complement inhibitor. In some aspects, agents useful for performing one or more of the methods are described.