丙烯酸琥珀酰亚胺-三聚乙二醇 | 1807518-71-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 丙烯酸琥珀酰亚胺-三聚乙二醇
• 英文名称: [3-(N-succinimidyl-oxy)-3-oxopropyl]triethylene glycol
• 英文别名: Hydroxy-PEG3-NHS；(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]propanoate
• CAS: 1807518-71-3
• 化学式: C₁₃H₂₁NO₈
• 分子量: 319.312
• InChiKey: KQGZCLFKXYOVGS-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：
  13
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.77
• 拓扑面积：
  112
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  丙烯酸琥珀酰亚胺-三聚乙二醇 在 吡啶 、 肼 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  [EN] PHARMACEUTICAL AGENT CONJUGATES TO MODULATE MACROPHAGE AND INFLAMMATORY FUNCTIONS AND USES THEREOF
  [FR] CONJUGUÉS D'AGENT PHARMACEUTIQUE POUR MODULER DES FONCTIONS MACROPHAGES ET INFLAMMATOIRES ET LEURS UTILISATIONS

  摘要：

  The present invention provides a means to target pharmaceutical agents to sites of inflammation within the body using a conjugate that includes the pharmaceutical agent linked by a cleavable linker to a polymer. The conjugate may also include a homing molecule, such as the targeting peptide CRV, linked to the polymer via a second linker. Specifically, the present invention provides the conjugates and methods of using these conjugates to reduce inflammation and treat inflammatory diseases.

  公开号：

  WO2023225597A2

文献信息

• Dimerization of a heat shock protein 90 inhibitor enhances inhibitory activity
  作者：Hendra Wahyudi、Yao Wang、Shelli R. McAlpine

  DOI：10.1039/c3ob41722k

  日期：——

  Heat shock protein 90 (hsp90) accounts for 1–2% of the total proteins in normal cells and it functions as a dimer. Hsp90 behaves as a molecular chaperone that folds, assembles, and stabilizes client proteins. We have developed a novel hsp90 inhibitor, and herein we describe the synthesis and biological activity of the dimerized variant of this inhibitor. Tethering a monomer inhibitor together produced a dimerized compound that more effectively inhibits hsp90 over the monomer.

  热休克蛋白 90（hsp90）占正常细胞蛋白质总量的 1-2%，它以二聚体的形式发挥作用。Hsp90 是一种分子伴侣，能折叠、组装和稳定客户蛋白。我们开发出了一种新型 hsp90 抑制剂，在此我们将介绍这种抑制剂二聚体变体的合成和生物活性。将单体抑制剂拴在一起产生的二聚化合物比单体抑制剂更有效地抑制 hsp90。
• INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING LFA-1
  申请人：Hoffmann-La Roche Inc.

  公开号：US20150065534A1

  公开（公告）日：2015-03-05

  The invention relates to compounds of formula (I), wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to LFA-1 integrin antagonists to target cells expressing LFA-1.

  本发明涉及公式（I）的化合物，其中R1，R2和n在详细说明和权利要求中有定义。特别是，本发明涉及公式I的化合物，用于制造和传递共轭基团，如小分子、肽、核酸、荧光基团和聚合物，这些共轭基团与LFA-1整合素拮抗剂连接，以靶向表达LFA-1的细胞。
• INSULIN RECEPTOR PARTIAL AGONISTS AND GLP-1 ANALOGUES
  申请人：MERCK SHARP & DOHME CORP.

  公开号：EP3922260A2

  公开（公告）日：2021-12-15

  The present invention provides compositions comprising insulin receptor partial agonists or insulin dimers in association with GLP-1 analogues (e.g., liraglutide) as well as methods for using the compositions for example, to treat or prevent diabetes or to decrease body weight.

  本发明提供了由胰岛素受体部分激动剂或胰岛素二聚体与GLP-1类似物（如利拉鲁肽）组成的组合物，以及使用这些组合物治疗或预防糖尿病或减轻体重的方法。
• INSULIN RECEPTOR PARTIAL AGONISTS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3221343B1

  公开（公告）日：2020-09-16
• [EN] PHARMACEUTICAL AGENT CONJUGATES TO MODULATE MACROPHAGE AND INFLAMMATORY FUNCTIONS AND USES THEREOF<br/>[FR] CONJUGUÉS D'AGENT PHARMACEUTIQUE POUR MODULER DES FONCTIONS MACROPHAGES ET INFLAMMATOIRES ET LEURS UTILISATIONS
  申请人：[en]REGENTS OF THE UNIVERSITY OF MINNESOTA

  公开号：WO2023225597A2

  公开（公告）日：2023-11-23

  The present invention provides a means to target pharmaceutical agents to sites of inflammation within the body using a conjugate that includes the pharmaceutical agent linked by a cleavable linker to a polymer. The conjugate may also include a homing molecule, such as the targeting peptide CRV, linked to the polymer via a second linker. Specifically, the present invention provides the conjugates and methods of using these conjugates to reduce inflammation and treat inflammatory diseases.