甲基-一聚乙二醇-NHS酯 | 1027371-75-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 甲基-一聚乙二醇-NHS酯
• 英文名称: 2,5-dioxopyrrolidin-1-yl 3-methoxypropanoate
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 3-methoxypropanoate
• CAS: 1027371-75-0
• 化学式: C₈H₁₁NO₅
• 分子量: 201.179
• InChiKey: GDPPBYZKFKEXML-UHFFFAOYSA-N

物化性质

• 沸点：
  292.8±42.0 °C(Predicted)
• 密度：
  1.31±0.1 g/cm3(Predicted)
• 溶解度：
  溶于二氯甲烷

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  14
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  72.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  甲基-一聚乙二醇-NHS酯 、 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 生成 (2S,3R)-3-hydroxy-4-(3-methoxypropanoylamino)-2-methyl-N-(5-methylhexyl)butanamide
  参考文献：
  名称：

  SYNTHESIS AND ANTICANCER ACTIVITY OF NEW ACTIN-TARGETING SMALL-MOLECULE AGENTS

  摘要：

  本发明提供了一种新型的双三胺类似物，可用于治疗各种类型的癌症。

  公开号：

  US20100217019A1
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 3-甲氧基丙酸 在 N,N'-二环己基碳二亚胺 作用下， 以 乙腈 为溶剂， 以67%的产率得到甲基-一聚乙二醇-NHS酯
  参考文献：
  名称：

  Rationally Simplified Bistramide Analog Reversibly Targets Actin Polymerization and Inhibits Cancer Progression in Vitro and in Vivo

  摘要：

  We describe structure-based design and chemical synthesis of a simplified analog of bistramide A, which potently and reversibly binds monomeric actin with a K(d) of 9.0 nM, depolymerizes filamentous actin in vitro and in A549 (nonsmall cell lung cancer) cells, inhibits growth of cancer cell lines in vitro at submicromolar concentrations, and significantly suppresses proliferation of A549 cells in a nude mice tumor xenograft model in terms of both tumor growth delay and average tumor volume. This study provides a conceptual framework for the design and development of new antiproliferative compounds that target cytoskeletal organization of cancer cells in vivo by a combination of reversible G-actin binding and effective F-actin severing.

  DOI：

  10.1021/ja101811x

文献信息

• BRYOSTATIN ANALOGUES AND METHODS OF MAKING AND USING THEREOF
  申请人：Keck Gary E.

  公开号：US20110269713A1

  公开（公告）日：2011-11-03

  Described herein are tricyclic macrolactones. The macrolactones have a high binding affinity for PKC. The compounds described herein can be used in a number of therapeutic applications including cancer and Alzheimer's prevention and treatment. The compounds described herein can also treat memory loss. Also described herein are methods for producing macrolactones. The methods permit the high-yield synthesis of macrolactones in fewer steps and with a higher degree of substitution and specificity.

  本文描述的是三环大环内酯。这些大环内酯对蛋白激酶C（PKC）具有很高的结合亲和力。本文描述的化合物可用于多种治疗应用，包括癌症和阿尔茨海默病的预防和治疗。本文描述的化合物还可以用于治疗记忆丧失。本文还描述了生产大环内酯的方法。这些方法允许在更少的步骤中以更高的置换度和特异性高产合成大环内酯。
• [EN] INSULIN RECEPTOR PARTIAL AGONISTS<br/>[FR] AGONISTES PARTIELS DU RÉCEPTEUR DE L'INSULINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2022046739A1

  公开（公告）日：2022-03-03

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

  本发明揭示了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。
• Therapeutic Nanomaterials
  申请人：University of Connecticut

  公开号：US20220133893A1

  公开（公告）日：2022-05-05

  Disclosed herein is a delivery vehicle based on DNA-inspired Janus based nanotubes (JBNTs) for anti-viral treatment. The nanoparticles (NPs) are based the JBNTs conjugated with targeting moieties such as small molecules, aptamers, and peptides.

  本文披露了一种基于DNA启发的Janus纳米管（JBNTs）的递送载体，用于抗病毒治疗。这些纳米粒子（NPs）是基于与靶向物质（如小分子、适配体和肽）结合的JBNTs。
• Complexes of Small-Interfering Nucleic Acids
  申请人：McManus Samuel P.

  公开号：US20110213013A1

  公开（公告）日：2011-09-01

  The present invention relates to complexes of small-interfering nucleic acids (siNA). Compositions of siNA suited for administration to a patient are described. Methods for delivering the compositions are also described.

  本发明涉及小干扰核酸（siNA）复合物。描述了适用于给患者治疗的siNA组合物。还描述了传递这些组合物的方法。
• CONJUGATES PF SMALL-INTERFERING NUCLEIC ACIDS
  申请人：McManus Samuel P.

  公开号：US20120100096A1

  公开（公告）日：2012-04-26

  The present invention relates to conjugates of small-interfering nucleic acids (siNA). Compositions of siNA suited for administration to a patient are described. Methods for delivering the compositions are also described.

  本发明涉及小干扰核酸（siNA）的结合物。本发明描述了适用于向患者施用的siNA组成物。还描述了传递这些组成物的方法。