H2N-PEG2000-OMe | 1160212-03-2

• 分子结构分类: 有机化合物
• 英文名称: H2N-PEG2000-OMe
• 英文别名: mPEG45-NH2；2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanamine
• CAS: 1160212-03-2
• 化学式: C₉₁H₁₈₅NO₄₅
• 分子量: 2013.45
• InChiKey: RNXJWXSVSSSMHG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -7.4
• 重原子数：
  137
• 可旋转键数：
  134
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  441
• 氢给体数：
  1
• 氢受体数：
  46

反应信息

• 作为反应物：
  描述：

  H2N-PEG2000-OMe 、 在 N,N'-二环己基碳二亚胺 、 DPTS 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 以78%的产率得到
  参考文献：
  名称：

  Impact of Hydrophobic Chain Composition on Amphiphilic Macromolecule Antiatherogenic Bioactivity

  摘要：

  Amphiphilic macromolecules (AMs) composed of sugar backbones modified with branched aliphatic chains and a poly(ethylene glycol) (PEG) tail can inhibit macrophage uptake of oxidized low-density lipoproteins (oxLDL), a major event underlying atherosclerosis development. Previous studies indicate that AM hydrophobic domains influence this bioactivity through interacting with macrophage scavenger receptors, which can contain basic and/or hydrophobic residues within their binding pockets. In this study, we compare two classes of AMs to investigate their ability to promote athero-protective potency via hydrogen-bonding or hydrophobic interactions with scavenger receptors. A series of ether-AMs, containing methoxy-terminated aliphatic arms capable of hydrogen-bonding, was synthesized. Compared to analogous AMs containing no ether moieties (alkyl-AMs), ether-AMs showed improved cytotoxicity profiles. Increasing AM hydrophobicity via incorporation of longer and/or alkyl-terminated hydrophobic chains yielded macromolecules with enhanced oxLDL uptake inhibition. These findings indicate that hydrophobic interactions and the length of AM aliphatic arms more significantly influence AM bioactivity than hydrogen-bonding.

  DOI：

  10.1021/bm500809f
• 作为产物：
  描述：

  在 一水合肼 作用下， 以 乙醇 为溶剂， 反应 12.0h， 以95%的产率得到H2N-PEG2000-OMe
  参考文献：
  名称：

  化学燃料驱动的瞬态聚合胶束纳米反应器，可逆捕集和反应加速

  摘要：

  在大多数合成纳米反应器系统中，催化产物不会迅速从纳米反应器中扩散出去，这导致催化效率低于预期。为了解决扩散问题，使用1-乙基-3-（3-二甲基氨基丙基）碳二亚胺（EDC）作为燃料，活化酯作为能量耗散单元，实现了瞬态聚合物胶束纳米反应器系统。这些证明了瞬态胶束的途径依赖性催化特性：在亚稳态阶段或瞬态胶束完全消散后，取决于EDC的重载，观察到或有效消除了产物抑制作用。

  DOI：

  10.1039/d1cc00726b

文献信息

• [EN] NOVEL 5-AMINO-2-THIOIMIDAZOLE COMPOUNDS AND THEIR USE<br/>[FR] NOUVEAUX COMPOSÉS 5-AMINO-2-THIO-IMIDAZOLES ET LEUR UTILISATION
  申请人：UNIV LILLE II DROIT & SANTE

  公开号：WO2017042380A1

  公开（公告）日：2017-03-16

  The present invention is directed to novel compounds of formula (I) pharmaceutically acceptable salts or solvates thereof, and their use.

  本发明涉及公式(I)的新化合物，其药用盐或溶剂，以及它们的用途。
• Acid-Triggered Release via dePEGylation of Fusogenic Liposomes Mediated by Heterobifunctional Phenyl-Substituted Vinyl Ethers with Tunable pH-Sensitivity
  作者：Hee-Kwon Kim、Jeroen Van den Bossche、Seok-Hee Hyun、David H. Thompson

  DOI：10.1021/bc300266y

  日期：2012.10.17

  lipopolymers were hydrolyzed under acidic conditions (pH 3.5 or 4.5) at rates that were dependent on the electron donating or withdrawing character of the α-phenyl vinyl ether substituent, while remaining stable at pH 7.4. Blending of these compounds with 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) in a 10:90 mPEG-PIVE-Lipid:DOPE ratio produced stable liposomes at neutral pH; however, acidification of

  已开发出一类新的具有可调酸敏感性的异双官能苯基取代乙烯基醚 (PIVE) 偶联剂。PIVE 化合物设计为在酸性条件下水解，水解速率可以通过合理选择苯环取代基而改变。这些试剂被掺入 2-甲氧基聚（乙二醇）PEG 共轭的 1,3-二十八烷基外消旋体中-甘油脂质产生酸可裂解的脂质聚合物 mPEG-[H-PIVE]-DOG、mPEG-[F-PIVE]-DOG、mPEG-[Me-PIVE]-DOG 和 mPEG-[MeO-PIVE]-DOG . 这些脂质聚合物在酸性条件（pH 3.5 或 4.5）下水解，水解速度取决于 α-苯基乙烯基醚取代基的给电子或吸电子特性，同时在 pH 7.4 下保持稳定。这些化合物与 1,2-dioleoyl- sn 的混合-甘油-3-磷酸乙醇胺 (DOPE) 以 10:90 mPEG-PIVE-LiPId:DOPE 的比例在中性 pH 下产生稳定的脂质体；然而，溶液的酸化
• Aza-dibenzocyclooctynes for fast and efficient enzyme PEGylation via copper-free (3+2) cycloaddition
  作者：Marjoke F. Debets、Sander S. van Berkel、Sanne Schoffelen、Floris P. J. T. Rutjes、Jan C. M. van Hest、Floris L. van Delft

  DOI：10.1039/b917797c

  日期：——

  A strained aza-dibenzocyclooctyne was prepared via a high-yielding synthetic route. Copper-free, strain-promoted click reaction with azides showed excellent kinetics, and a functionalised aza-cyclooctyne was applied in fast and efficient PEGylation of enzymes.

  通过高产合成路线制备了一种含杂二苯并环辛炔。无铜、菌株促进的叠氮化物点击反应显示出卓越的动力学性能，功能化的氮杂环辛炔被应用于酶的快速高效 PEG 化。
• DNA–polymer conjugates <i>via</i> the graft-through polymerisation of native DNA in water
  作者：Lucy A. Arkinstall、Jonathan T. Husband、Thomas R. Wilks、Jeffrey C. Foster、Rachel K. O'Reilly

  DOI：10.1039/d0cc08008j

  日期：——

  The direct, graft-through, ring-opening metathesis polymerisation (ROMP) of unprotected DNA macromonomers is reported.

  报道了未保护的DNA大分子单体的直接、嫁接、环开放的转化聚合（ROMP）。
• Wavelength‐Orthogonal Stiffening of Hydrogel Networks with Visible Light
  作者：Vinh X. Truong、Julian Bachmann、Andreas‐Neil Unterreiner、James P. Blinco、Christopher Barner‐Kowollik

  DOI：10.1002/anie.202113076

  日期：2022.4.4

  It's So Clearly Visible: Hydrogels can be formed by exclusively visible-light irradiation with two colours of light, with each colour allowing mechanical stiffening of the gel independent of the order in which each colour is applied. Driven by mild [2+2] cycloadditions with halochromic properties, the photoreactivity of the reactions in water can be controlled by a photoacid generator.

  清晰可见：水凝胶可以通过两种颜色的光进行专门的可见光照射来形成，每种颜色都可以使凝胶机械硬化，而与每种颜色的施加顺序无关。在具有卤色特性的温和[2+2]环加成反应的驱动下，水中反应的光反应性可以通过光致产酸剂来控制。