O1-(二甲氧基三苯甲基)HEXA乙烯GLYCOL | 123706-69-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 中文名称: O1-(二甲氧基三苯甲基)HEXA乙烯GLYCOL
• 英文名称: 17-<(4,4'-dimethoxytrityl)oxy>-3,6,9,12,15-pentaoxaheptadecan-1-ol
• 英文别名: O-(4,4'-dimethoxytrityl)hexaethyleneglycol；1-(4,4'-dimethoxytrityl)hexaethylene glycol；18-O-dimethoxytrityl hexaethylene glycol；DMT-HEG；1-hydroxy-17-[(4,4'-bismethoxytrityl)oxy]-3,6,9,12,15-pentaoxaheptadecane；(4,4'-Dimethoxytrityloxy)-hexaethylene glycol；DMTO-hexaethylene glycol；O1-(Dimethoxytrityl)hexaethylene glycol；2-[2-[2-[2-[2-[2-[bis(4-methoxyphenyl)-phenylmethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol
• CAS: 123706-69-4
• 化学式: C₃₃H₄₄O₉
• 分子量: 584.707
• InChiKey: TZXARFLYKYWWKC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  42
• 可旋转键数：
  23
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  94.1
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  O1-(二甲氧基三苯甲基)HEXA乙烯GLYCOL 在 4-二甲氨基吡啶 、 N,N'-二环己基碳二亚胺 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Biologically active oligodeoxyribonucleotides—IX.1 Synthesis and anti-HIV-1 activity of hexadeoxyribonucleotides, TGGGAG, bearing 3′- and 5′-end-modification

  摘要：

  We have determined that hexadeoxyribonucleotides (5'TGGGAG3'), with modified aromatic groups such as a trityl group at the 5'-end, have anti-HIV-1 activity in vitro. The 6-mer bearing a 3,4-dibenzyloxybenzyl (3,4-DBB) group at the 5'-end had the most potent activity and the least cytotoxicity. When the 3'-end of the 5'-(3,4-DBB)-modified 6-mer was substituted with a 2-hydroxyethylphosphate, a 2-hydroxyethylthiophosphate, or a methylphosphate group at the 3'-end, anti-HIV-1 activity increased. Moreover, among various 3'- and 5'-end-modified 6-mers that were tested, the 6-mer (R-95288) bearing a 3,4-DBB group at the 5'-end and a 2-hydroxyethylphosphate group at the 3'-end was the most stable, when incubated with mouse, rat, or human plasma. Therefore, R-95288 was chosen as the best candidate for possible use in therapy on the basis of its anti-HIV-1 activity. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00161-2
• 作为产物：
  描述：

  在 吡啶 作用下， 生成 O1-(二甲氧基三苯甲基)HEXA乙烯GLYCOL
  参考文献：
  名称：

  Synthesis of guanosine 5′-conjugates and their use as initiator molecules for transcription priming

  摘要：

  我们合成了两种与生物素化腺苷部分相连的鸟苷衍生物，采用了两种不同的策略，一种是在固相上进行合成步骤，另一种则完全在溶液中进行。合成的衍生物在转录引物实验中被证明可以作为引发分子使用。引入效率被确定为大约2%。尽管这个值相对较低，但在选择实验中使用其中任何一种分子似乎都是合理的。基本上，可以生成序列复杂度为10^15到10^16的RNA文库。用我们的引发分子标记这样的文库仍然可以产生10^13到10^14个标记/功能化序列，从而提供足够的序列空间用于选择。

  DOI：

  10.1039/b716151d

文献信息

• ADJUVANT IN THE FORM OF A LIPID-MODIFIED NUCLEIC ACID
  申请人：Hoerr Ingmar

  公开号：US20070280929A1

  公开（公告）日：2007-12-06

  The present invention relates to an immune-stimulating adjuvant in the form of a lipid-modified nucleic acid, optionally in combination with further adjuvants. The invention relates further to a pharmaceutical composition and to a vaccine, each containing an immune-stimulating adjuvant according to the invention, at least one active ingredient and optionally a pharmaceutically acceptable carrier and/or further auxiliary substances and additives and/or further adjuvants. The present invention relates likewise to the use of the pharmaceutical composition according to the invention and of the vaccine according to the invention for the treatment of infectious diseases or cancer diseases. Likewise, the present invention includes the use of the immune-stimulating adjuvant according to the invention in the preparation of a pharmaceutical composition for the treatment of cancer diseases or infectious diseases.

  本发明涉及一种免疫刺激佐剂，其形式为脂质修饰的核酸，可选地与其他佐剂结合。该发明还涉及一种含有根据本发明的免疫刺激佐剂、至少一种活性成分以及可选的药用载体和/或其他辅助物质和添加剂和/或其他佐剂的药物组合物和疫苗。本发明还涉及根据本发明的药物组合物和疫苗用于治疗传染病或癌症的用途。同样，本发明包括根据本发明的免疫刺激佐剂用于制备用于治疗癌症或传染病的药物组合物的用途。
• NUCLEIC ACID OF FORMULA (I): GlXmGn, OR (II): ClXmCn, IN PARTICULAR AS AN IMMUNE-STIMULATING AGENT/ADJUVANT
  申请人：CureVac AG

  公开号：US20200016264A1

  公开（公告）日：2020-01-16

  The present invention relates to a nucleic acid of the general formula (I): G l X m G n , or (II): C l X m C n , which may be modified by a lipid. The nucleic acid of the invention acts as an immune-stimulating agent inducing the innate immune response. The invention relates further to a pharmaceutical composition (in a first embodiment), each containing an immune-stimulating agent according to the invention in combination with a pharmaceutically active carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). In another embodiment, the inventive nucleic acid is combined with at least one pharmaceutically active component, a pharmaceutically acceptable carrier/vehicle (and, optionally, further auxiliary substances, additives and/or further adjuvants). Accordingly, the present invention is directed to a vaccine, which corresponds to a pharmaceutical composition of the invention (second embodiment), wherein the pharmaceutically active component induces a specific immune response (e.g. an antigen). The present invention relates likewise to the use of a nucleic acid of the invention or a pharmaceutical composition according to the invention for the treatment of infectious diseases, autoimmune diseases, allergies or cancer diseases.

  本发明涉及一般式(I)：G l X m G n 或(II)：C l X m C n的核酸，该核酸可以通过脂质进行修饰。本发明的核酸作为免疫刺激剂，诱导先天免疫应答。本发明还涉及一种药物组合物（在第一实施例中），每种组合物包含本发明的免疫刺激剂与药用活性载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）的组合。在另一实施例中，创新的核酸与至少一种药用活性成分、药用可接受的载体/载体（以及可选的进一步辅助物质、添加剂和/或进一步佐剂）结合。因此，本发明涉及一种疫苗，该疫苗对应于本发明的药物组合物（第二实施例），其中药用活性成分诱导特异免疫应答（例如抗原）。本发明同样涉及利用本发明的核酸或药物组合物治疗传染病、自身免疫疾病、过敏或癌症疾病。
• [EN] OLIGONUCLEOTIDE SYNTHESIS ON SOLID SUPPORT<br/>[FR] SYNTHÈSE D'OLIGONUCLÉOTIDES SUR SUPPORT SOLIDE
  申请人：INTEGRATED DNA TECH INC

  公开号：WO2021173615A1

  公开（公告）日：2021-09-02

  Functionalized solid supports are useful in the synthesis of oligonucleotides. The functionalized solid supports contain an extended linker to a terminal functional group or a first nucleotide or nucleoside moiety. The extended linker permits oligonucleotide synthesis to take place at a greater distance from the solid support with greater efficiency.

  功能化固体支持物在寡核苷酸的合成中非常有用。这些功能化固体支持物包含一个延长的连接器，连接到一个终端功能基团或第一个核苷酸或核苷苷基团。延长的连接器使寡核苷酸的合成能够在距固体支持物更远的位置上更有效地进行。
• A fibre-optic biosensor for detection of microbial contamination
  作者：Amer Almadidy、James Watterson、Paul AE Piunno、Inge V Foulds、Paul A Horgen、Ulrich Krull

  DOI：10.1139/v03-070

  日期：2003.5.1

  A fibre-optic biosensor is described for detection of genomic target sequences from Escherichia coli. A small portion of the LacZ DNA sequence is the basis for selection of DNA probe molecules that are produced by automated nucleic acid synthesis on the surface of optical fibres. Fluorescent intercalating agents are used to report the presence of hybridization events with target strands. This work reviews the fundamental design criteria for development of nucleic acid biosensors and reports a preliminary exploration of the use of the biosensor for detection of sequences that mark the presence of E. coli. The research work includes consideration of the length of the strands and non-selective binding interactions that can potentially block the selective chemistry or create background signals. The biosensors were able to detect genomic targets from E. coli at a picomole level in a time of a few minutes, and dozens of cycles of use have been demonstrated. In a step towards the preparation of a completely self-contained sensor technology, a new intercalating dye known as SYBR 101 (Molecular Probes, Inc.) has been end-labelled to the LacZ nucleic acid probe, to examine whether dye tethered onto an oligonucleotide terminus could fluorimetrically transduce the formation of hybrids. The results obtained from experiments in solution indicate that the use of tethered dye provides fluorescence signals that are due to hybridization, and that this process is functional even in the presence of a high concentration of non-selective background DNA obtained from sonicated salmon sperm. Key words: biosensor, DNA, fibre optic, hybridization, fluorescence, pathogen, E. coli.

  本文介绍了一种光纤生物传感器，用于检测大肠杆菌基因组目标序列。LacZ DNA序列的一小部分是基于选择在光纤表面自动核酸合成产生的DNA探针分子的基础。荧光插入剂用于报告与目标链的杂交事件的存在。本研究回顾了核酸生物传感器开发的基本设计标准，并报告了生物传感器用于检测标记大肠杆菌存在的序列的初步探索。研究工作包括考虑链的长度和非选择性结合相互作用，这可能会阻止选择性化学或创建背景信号。生物传感器能够在几分钟内以皮摩尔级别检测到来自大肠杆菌的基因组目标，并已证明可以进行数十个使用周期。为了准备完全自包含的传感器技术，一种名为SYBR 101（Molecular Probes，Inc.）的新型插入染料已被端标记到LacZ核酸探针上，以检查染料是否能够荧光转导杂交物的形成。在溶液实验中获得的结果表明，使用连接染料提供由杂交引起的荧光信号，并且即使存在来自声化鲑鱼精子的高浓度非选择性背景DNA，此过程也是功能性的。关键词：生物传感器，DNA，光纤，杂交，荧光，病原体，大肠杆菌。
• Vascular endothelial growth factor (VEGF) nucleic acid ligand complexes
  申请人：Gilead Sciences, Inc.

  公开号：US20030114404A1

  公开（公告）日：2003-06-19

  This invention discloses a method for preparing a complex comprised of a VEGF Nucleic Acid Ligand and a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound by identifying a VEGF Nucleic Acid Ligand by SELEX methodology and associating the VEGF Nucleic Acid Ligand with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further discloses Complexes comprising one or more VEGF Nucleic Acid Ligands in association with a Non-Immunogenic, High Molecular Weight Compound or Lipophilic Compound. The invention further includes a Lipid construct comprising a VEGF Nucleic Acid Ligand or Complex and methods for making the same.

  这项发明揭示了一种制备VEGF核酸配体和非免疫原性、高分子量化合物或亲脂性化合物复合物的方法，通过SELEX方法识别VEGF核酸配体，并将其与非免疫原性、高分子量化合物或亲脂性化合物结合。该发明进一步揭示了包含一个或多个VEGF核酸配体与非免疫原性、高分子量化合物或亲脂性化合物结合的复合物。该发明还包括一种脂质构造物，包括VEGF核酸配体或复合物，以及制备该构造物的方法。