N-Hydroxysuccinimidyl-methylthioacetat | 51244-88-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: N-Hydroxysuccinimidyl-methylthioacetat
• 英文别名: N-succinimidyl 2-methylthioacetate；N-methylsulfanylacetoxy-succinimide；Aceticc acid, 2-(methylthio)-, 2,5-dioxo-1-pyrrolidinyl ester；(2,5-dioxopyrrolidin-1-yl) 2-methylsulfanylacetate
• CAS: 51244-88-3
• 化学式: C₇H₉NO₄S
• 分子量: 203.219
• InChiKey: JQUYACFIADHYOD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  89
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-Hydroxysuccinimidyl-methylthioacetat 、 7-氨基头孢烷酸 在 三乙胺 作用下， 生成 7-Methylmercaptoacetylamino-cephalosporadesinsaeure
  参考文献：
  名称：

  A new parenteral cephalosporin. SK&F 59962: 7-trifluoromethylthioacetamido-3-(1-methyl-1H-tetrazol-5-ylthiomethyl)-3-cephem-4-carboxylic acid. Chemistry and structure activity relationships.

  摘要：

  本研究介绍了一系列头孢菌素的合成、微生物学特征和在实验室动物体内的有效性，这些头孢菌素的 7-酰基取代基来自甲硫基乙酸。所研究的结构-活性关系包括侧链硫原子氧化、氟取代（侧链）甲基氢和硫杂环取代 3-乙酰氧基取代基的影响。其中一种衍生物，即 7-三氟甲基硫代乙酰氨基-3-（1-甲基-1H-四唑-5-基硫甲基）-3-头孢-4-羧酸（SK&F 59962），在体外和体内都具有出色的抗菌活性。

  DOI：

  10.7164/antibiotics.28.463

文献信息

• Stilbene Derivatives And Their Use For Binding And Imaging Amyloid Plaques
  申请人：Kung F. Hank

  公开号：US20080108840A1

  公开（公告）日：2008-05-08

  This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

  本发明涉及成像淀粉样沉积物的方法、标记化合物以及制备标记化合物用于成像淀粉样沉积物的方法。本发明还涉及化合物及制备化合物以抑制淀粉样蛋白聚集形成淀粉样沉积物的方法，以及将治疗剂输送到淀粉样沉积物的方法。
• SINGLE-STRANDED NUCLEIC ACID MOLECULE FOR REGULATING EXPRESSION OF GENE HAVING DELIVERING FUNCTION
  申请人：Bonac Corporation

  公开号：US20150105443A1

  公开（公告）日：2015-04-16

  The invention provides a single-stranded nucleic acid capable of inhibiting expression of a target gene having a delivery function. The nucleic acid contains, from the 5′-side to the 3′-side, a 5′-side region (Xc), a linker region (Lx), an inner region (Z), a linker region (Ly) and a 3′-side region (Yc) in this order, wherein the inner region (Z) is constituted by linkage of the inner 5′-side region (X) and the inner 3′-side region (Y), the 5′-side region (Xc) is complementary to the inner 5′-side region (X), the 3′-side region (Yc) is complementary to the inner 3′-side region (Y), at least one of the inner region (Z), the 5′-side region (Xc) and the 3′-side region (Yc) comprises an expression inhibitory sequence that inhibits expression of a target gene, and at least one of the 5′-terminus, the 3′-terminus, the linker region (Lx) and the linker region (Ly) is bound to a bio-related substance.

  本发明提供了一种单链核酸，具有抑制具有递送功能的靶基因表达的能力。该核酸包含从5'-端到3'-端的5'-端区域（Xc）、连接区域（Lx）、内部区域（Z）、连接区域（Ly）和3'-端区域（Yc），其中内部区域（Z）由内部5'-端区域（X）和内部3'-端区域（Y）的连接构成，5'-端区域（Xc）与内部5'-端区域（X）互补，3'-端区域（Yc）与内部3'-端区域（Y）互补，至少其中之一的内部区域（Z）、5'-端区域（Xc）和3'-端区域（Yc）包含抑制靶基因表达的表达抑制序列，而5'-端、3'-端、连接区域（Lx）和连接区域（Ly）中至少有一个与生物相关物质结合。
• Design and synthesis of dinucleotide 5′-triphosphates with expanded functionality
  作者：Tatiana V. Abramova、Svetlana V. Vasileva、Ludmila S. Koroleva、Nina S. Kasatkina、Vladimir N. Silnikov

  DOI：10.1016/j.bmc.2008.09.029

  日期：2008.10

  We propose the new approach to the synthesis of 5 '-triphosphate derivatives of natural and modified dinucleotides with expanded functionality. Our strategy includes the combination of the solution phase synthesis of necessary dimers using the wide range of nucleic acids chemistry methods and the subsequent introduction of the triphosphate residue. A number of the new potential substrates for the template dependent synthesis of nucleic acids with expanded functionality are obtained, namely, 5 '-triphosphates of dinucleotides containing the functionally active groups in heterocyclic bases, in carbohydrate -phosphate backbone, and the groups mimicking the residues of natural amino acids. The abilities of the proposed synthetic route are also demonstrated by the synthesis of 5 '-triphosphates of dinucleotides with modified carbohydrate-phosphate backbone. (C) 2008 Elsevier Ltd. All rights reserved.
• MULTI-ARMED, MONOFUNCTIONAL, AND HYDROLYTICALLY STABLE DERIVATIVES OF POLY(ETHYLENE GLYCOL) AND RELATED POLYMERS FOR MODIFICATION OF SURFACES AND MOLECULES
  申请人：NEKTAR THERAPEUTICS

  公开号：US20130177961A1

  公开（公告）日：2013-07-11

  Multi-armed, monofunctional, and hydrolytically stable polymers are described having the structure wherein Z is a moiety that can be activated for attachment to biologically active molecules such as proteins and wherein P and Q represent linkage fragments that join polymer arms poly a and poly b , respectively, to central carbon atom, C, by hydrolytically stable linkages in the absence of aromatic rings in the linkage fragments. R typically is hydrogen or methyl, but can be a linkage fragment that includes another polymer arm. A specific example is an mPEG disubstituted lysine having the structure where mPEG a and mPEG b have the structure CH 3 O—(CH 2 CH 2 O) n CH 2 CH 2 — where n may be the same or different for poly a - and poly b - and can be from 1 to about 1,150 to provide molecular weights of from about 100 to 100,000.
• NOVEL ANTI-DPEP3 ANTIBODIES AND METHODS OF USE
  申请人：AbbVie Stemcentrx LLC

  公开号：US20170044271A1

  公开（公告）日：2017-02-16

  Provided herein are novel anti-DPEP3 antibodies and antibody drug conjugates (ADC), including derivatives thereof, and methods of using the same to treat proliferative disorders.