双琥珀酰亚胺酯-PEG3 | 1314378-16-9

• 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: 双琥珀酰亚胺酯-PEG3
• 英文名称: 3,6,9-trioxa-undecan-1,11-dicarboxylic acid bis-N-succinimidyl ester
• 英文别名: Bis-PEG3-NHS Ester；(2,5-dioxopyrrolidin-1-yl) 3-[2-[2-[3-(2,5-dioxopyrrolidin-1-yl)oxy-3-oxopropoxy]ethoxy]ethoxy]propanoate
• CAS: 1314378-16-9
• 化学式: C₁₈H₂₄N₂O₁₁
• 分子量: 444.395
• InChiKey: OPGNUERFYQLUNP-UHFFFAOYSA-N

物化性质

• 沸点：
  577.4±60.0 °C(Predicted)
• 密度：
  1.42±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.3
• 重原子数：
  31
• 可旋转键数：
  16
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  155
• 氢给体数：
  0
• 氢受体数：
  11

制备方法与用途

生物活性

Bis-PEG3-NHS ester 是一种不可降解的含 3 个单元 PEG 的 linker，可用于合成抗体偶联药物 (ADC) 。

靶点

Non-cleavable

反应信息

• 作为反应物：
  描述：

  (4-(6-methyl-1,2,4,5-tetrazin-3-yl)phenyl)methanamine 、 双琥珀酰亚胺酯-PEG3 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 以62%的产率得到Methyltetrazine-amino-PEG3-CH2CH2COONHS
  参考文献：
  名称：

  In situ activation of a doxorubicin prodrug using imaging-capable nanoparticles

  摘要：

  描述了一种使用荧光标记的磁性氧化铁纳米颗粒进行图像引导的前药激活的一般策略。

  DOI：

  10.1039/c6cc01024e

文献信息

• [EN] INSULIN RECEPTOR PARTIAL AGONISTS AND GLP-1 ANALOGUES<br/>[FR] AGONISTES PARTIELS DU RÉCEPTEUR DE L'INSULINE ET ANALOGUES DU GLP-1
  申请人：MERCK SHARP & DOHME

  公开号：WO2017205191A1

  公开（公告）日：2017-11-30

  The present invention provides compositions comprising insulin receptor partial agonists 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.

  本发明提供了包含胰岛素受体部分激动剂与GLP-1类似物（例如利拉鲁肽）的组合物，以及使用该组合物的方法，例如用于治疗或预防糖尿病或减轻体重。
• Crosslinked gels comprising polyalkyleneimines, and their uses as medical devices
  申请人：Stockman E. Kenneth

  公开号：US20070196454A1

  公开（公告）日：2007-08-23

  One aspect of the present invention generally relates to methods of sealing a wound or tissue plane or filling a void splace. In a preferred embodiment, the wound is an ophthalmic, pleural or dural wound. In certain instances, the compositions used to seal the wound or tissue plane comprises a polyalkyleneamine. In a preferred embodiment, the polyalkyleneamine is polyethyleneimine. Treatment of the polyethyleneimine with a cross-linking reagent causes the polyethyleneimine polymers to polymerize forming a seal. In certain instances, the cross-linking reagent is a polyethylene glycol having reactive terminal groups. In certain instances, the reactive terminal groups are activated esters, such as N-hydroxy succinimide ester. In certain instances, the reactive terminal groups are isocyanates. In certain instances, the polyethyleneimine has a lysine, cysteine, isocysteine or other nucleophilic group attached to the periphery of the polymer. In certain instances, the polyethyleneimine is mixed with a second polymer, such as a polyethylene glycol containing nucleophilic groups. In certain instances, the compositions used to seal the wound or tissue plane are formed by reacting a polyalkyleneamine bearing electrophilic groups with a cross-linking reagent containing nucleophilic groups. In certain instances, the electrophilic groups on the polyalkyleneamine are activated esters, such as N-hydroxy succinimide ester. In certain instances, the compositions used to seal the wound or tissue plane are formed by reacting a polyalkyleneamine bearing photopolymerizable groups with ultraviolet or visibile light. Compositions used to seal the wound which contain PEI or a derivative of PEI are found to adhere tightly to the tissue. Other aspects of the present invention relate to methods of filling a void of a patient or adhering tissue. In certain instances, the methods use a polyalkyleneamine. In a preferred embodiment, the polyalkyleneamine is polyethyleneimine. Another aspect of the present invention relates to a polymeric composition formed by exposing a polyalkyleneamine to an activated polyalkylene glycol. In certain instances, the composition is attached to mammalian tissue.

  本发明的一个方面通常涉及封闭伤口或组织平面或填充空隙的方法。在一个优选实施例中，伤口是眼科、胸膜或硬脑膜伤口。在某些情况下，用于封闭伤口或组织平面的组合物包括聚烷胺。在一个优选实施例中，聚烷胺是聚乙烯亚胺。用交联试剂处理聚乙烯亚胺会导致聚乙烯亚胺聚合物聚合形成密封。在某些情况下，交联试剂是具有反应末端基团的聚乙二醇。在某些情况下，反应末端基团是活化酯，如N-羟基琥珀酰亚胺酯。在某些情况下，反应末端基团是异氰酸酯。在某些情况下，聚乙烯亚胺具有赖氨酸、半胱氨酸、异半胱氨酸或其他亲核基团附着在聚合物的周边。在某些情况下，聚乙烯亚胺与第二聚合物混合，如含有亲核基团的聚乙二醇。在某些情况下，用于封闭伤口或组织平面的组合物是通过将具有亲电子基团的聚烷胺与含有亲核基团的交联试剂反应形成的。在某些情况下，聚烷胺上的亲电子基团是活化酯，如N-羟基琥珀酰亚胺酯。在某些情况下，用于封闭伤口或组织平面的组合物是通过将具有光聚合基团的聚烷胺与紫外光或可见光反应形成的。发现含有PEI或PEI衍生物的用于封闭伤口的组合物能够紧密粘附在组织上。本发明的其他方面涉及填充患者空隙或粘附组织的方法。在某些情况下，这些方法使用聚烷胺。在一个优选实施例中，聚烷胺是聚乙烯亚胺。本发明的另一个方面涉及通过将聚烷胺暴露于活化聚乙烯醇而形成的聚合物组合物。在某些情况下，这种组合物附着在哺乳动物组织上。
• 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：US10017556B2

  公开（公告）日：2018-07-10

  Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.

  本研究公开了可作为胰岛素受体部分激动剂的胰岛素二聚体和胰岛素类似物二聚体。
• Insulin receptor partial agonists and GLP-1 analogues
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10953076B2

  公开（公告）日：2021-03-23

  The present invention provides compositions comprising insulin receptor partial agonists 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.

  本发明提供了包含胰岛素受体部分激动剂与 GLP-1 类似物（如利拉鲁肽）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。