3H-吡唑并[1,5-b][1,2,4]三唑-6,7-二胺,2-甲基- | 83306-17-6

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 中文名称: 3H-吡唑并[1,5-b][1,2,4]三唑-6,7-二胺,2-甲基-
• 中文别名: 1-[1-氧代-3-(2-吡啶基硫代)丙氧基]吡咯烷-2,5-二酮
• 英文名称: 1-(1-Oxo-3-(2-pyridylthio)propoxy)pyrrolidine-2,5-dione
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 3-pyridin-2-ylsulfanylpropanoate
• CAS: 83306-17-6
• 化学式: C₁₂H₁₂N₂O₄S
• 分子量: 280.3
• InChiKey: QMXCRMQIVATQMR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  19
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  102
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• ANTIBODY DRUG
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1731168A1

  公开（公告）日：2006-12-13

  The present invention provides an agent for improving the blood stability of an endogenous ligand, which comprises an antibody that has affinity to the mammalian endogenous ligand but substantially does not neutralize the same, and the above-described agent for the prophylaxis and/or treatment for a disease for which an increase in the blood concentration of the endogenous ligand and/or an prolonged blood half-life is prophylactically or therapeutically effective. Provided that the above-described agent is administered alone to a mammal without co-administering the same or substantially the same compound as the endogenous ligand, the blood stability of the endogenous ligand increases and the receptor activity-regulatory action thereof is enhanced.

  本发明提供了一种用于改善内源配体血液稳定性的药剂，包括一种具有亲和力与哺乳动物内源配体结合但实质上不中和其的抗体，以及上述药剂用于预防和/或治疗增加内源配体血液浓度和/或延长血液半衰期对预防或治疗有效的疾病。只要上述药剂单独给哺乳动物使用，而不与内源配体相同或实质相同的化合物联合给药，内源配体的血液稳定性增加，其受体活性调节作用得到增强。
• [EN] BORONATE-MEDIATED DELIVERY OF MOLECULES INTO CELLS<br/>[FR] ADMINISTRATION DE MÉDICAMENT MÉDIÉE PAR LES BORONATE
  申请人：WISCONSIN ALUMNI RES FOUND

  公开号：WO2013110005A1

  公开（公告）日：2013-07-25

  Methods for enhancing cellular uptake of cargo molecules by boronating the cargo molecule, particularly with one or more phenylboronic acid groups. Cellular uptake includes at least partial uptake into the cytosol. Boronation includes ligating, crosslinking or otherwise bonding one or more phenylboronic acids substituted to contain a reactive group to a cargo molecule. Boronation also includes ligating, crosslinking or otherwise bonding a phenylboronated oligopeptide to a cargo molecule. The phenylboronate groups are optionally conjugated to the cargo molecule via linking moieties that can be selectively cleaved. The invention includes certain phenylboronates which are boronation reagents, certain boronated oligopeptides and certain boronated peptides and proteins. The invention also includes kits for enhancing cellular uptake of cargo molecules by boronation with one or more phenylboronates or boronated oligopeptides.

  增强货物分子细胞摄取的方法，通过将货物分子硼酸化，特别是与一个或多个苯硼酸基团硼酸化。细胞摄取至少包括部分摄取到细胞质中。硼酸化包括将一个或多个含有反应基团的取代苯硼酸与货物分子连接、交联或以其他方式键合。硼酸化还包括将苯硼酸化的寡肽与货物分子连接、交联或以其他方式键合。可选地，苯硼酸基团通过可以选择性切割的连接基团与货物分子连接。本发明包括某些作为硼酸化试剂的苯硼酸、某些硼酸化的寡肽以及某些硼酸化的肽和蛋白质。本发明还包括通过用一种或多种苯硼酸或硼酸化寡肽硼酸化来增强货物分子细胞摄取的试剂盒。
• [EN] DITHIOAMINE REDUCING AGENTS<br/>[FR] AGENTS RÉDUCTEURS DITHIOAMINE
  申请人：WISCONSIN ALUMNI RES FOUND

  公开号：WO2013123382A1

  公开（公告）日：2013-08-22

  Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention can be employed to regulate protein function in proteins in which a sulfhydryl group is associated with biological activity. Reducing agents of this invention can prevent inactivation of a given protein or enhance activation of a given protein or other biological molecule in vitro and/or in vivo. Reducing agents of this invention can prevent or reduce oxidation of cysteine residues in proteins and prevent the formation of reduced activity protein dimers (or other oligomers). Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents.

  硫胺类还原剂可用于还原二硫键。该发明的还原剂可用于还原二硫键，特别是蛋白质中的二硫键，或者预防二硫键的形成，特别是在蛋白质和其他生物分子中。该发明的还原剂可用于调节蛋白质功能，其中巯基与生物活性相关。该发明的还原剂可防止给定蛋白质的失活，或增强给定蛋白质或其他生物分子的活化，无论是在体外还是体内。该发明的还原剂可预防或减少蛋白质中半胱氨酸残基的氧化，并防止降低活性蛋白质二聚体（或其他寡聚体）的形成。该发明的还原剂适用于各种生物应用，特别是作为研究和合成试剂。
• Delivery of compounds with rehydrated blood cells
  申请人：Nichols C. Timothy

  公开号：US20050025748A1

  公开（公告）日：2005-02-03

  Fixed-dried blood cells carrying an active agent are described, along with methods of making the same, methods of using the same, and compositions containing the same. The blood cells may be red blood cells or blood platelets.

  描述了携带活性剂的固定干燥血细胞，以及制备这些血细胞的方法、使用这些血细胞的方法以及含有这些血细胞的组合物。这些血细胞可以是红细胞或血小板。
• Novel rare earth metal cryptates which are not very sensitive to the fluorescence quenching
  申请人：——

  公开号：US20040092726A1

  公开（公告）日：2004-05-13

  The invention relates to a process for reducing the fluorescence quenching caused by the measuring medium in a fluorescence assay, by introducing into said medium of rare earth metal cryptates which are not very sensitive to this fluorescence quenching, said rare earth metal cryptates comprising at least one pyridine radical which is substituted one or more times or unsubstituted. The invention also relates to novel rare earth metal cryptates which are not very sensitive to the fluorescence quenching caused by the measuring medium.

  该发明涉及一种减少荧光测定中测量介质引起的荧光猝灭的过程，通过向该介质中引入对该荧光猝灭不太敏感的稀土金属螯合物，所述稀土金属螯合物包括至少一个吡啶基，该吡啶基被取代一次或多次或未取代。该发明还涉及一种新型对测量介质引起的荧光猝灭不太敏感的稀土金属螯合物。