L-Lys-ε-(stearoyl)-N1-spermine

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: L-Lys-ε-(stearoyl)-N1-spermine
• 英文别名: N-[(5S)-5-amino-6-[3-[4-(3-aminopropylamino)butylamino]propylamino]-6-oxohexyl]octadecanamide
• 化学式: C₃₄H₇₂N₆O₂
• 分子量: 596.985
• InChiKey: OIYSMVCNCLHLDA-YTTGMZPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.1
• 重原子数：
  42
• 可旋转键数：
  34
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  134
• 氢给体数：
  6
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  精胺 在 palladium on activated charcoal 盐酸 、 氢气 、 三乙胺 作用下， 以 甲醇 、 乙醇 、 二氯甲烷 为溶剂， 反应 23.5h， 生成 L-Lys-ε-(stearoyl)-N1-spermine
  参考文献：
  名称：

  Lysine–spermine conjugates: hydrophobic polyamine amides as potent lipopolysaccharide sequestrants

  摘要：

  Lipopolysaccharides (LPS), otherwise termed `endotoxins' are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of `Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammatory processes by targeting lipopolysaccharide do not exist at the present time. We have defined the pharmacophore necessary for small molecules to specifically bind and neutralize LPS and, using animal models of sepsis, have shown that the sequestration of circulatory LPS by small molecules is a therapeutically viable strategy. In this paper, the interactions of a focused library of lysine-spermine conjugates with lipopolysaccharide (LPS) have been characterized. Lysine-spermine conjugates with the epsilon-amino terminus of the lysinyl moiety derivatized with long-chain aliphatic hydrophobic substituents in acyl or alkyl linkage bind and neutralize bacterial lipopolysaccharides, and may be of use in the prevention or treatment of endotoxic shock states. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2005.01.038

文献信息

• Methods and compositions for treatment of demyelinating diseases
  申请人：Pathologica LLC

  公开号：US10350178B2

  公开（公告）日：2019-07-16

  Disclosed herein is a method of prevention of progression of a multiple sclerosis in a patient, comprising the administration of methylglyoxal bis(guanylhydrazone) (MGBG) to the patient in need thereof. Also disclosed herein is a method of prevention or reduction in severity of the initiation phase of autoimmune response in a patient having multiple sclerosis, comprising the administration of MGBG to the patient in need thereof.

  本文公开了一种预防多发性硬化症患者病情恶化的方法，包括向有需要的患者施用甲基乙二醛双（鸟苷酸腙）（MGBG）。本文还公开了一种预防多发性硬化症患者自身免疫反应起始阶段或减轻其严重程度的方法，包括对有需要的患者施用 MGBG。
• PHARMACEUTICAL FOR ORAL DELIVERY COMPRISING MGBG AND METHODS OF TREATING DISEASE
  申请人：McKearn John

  公开号：US20110112199A1

  公开（公告）日：2011-05-12

  Disclosed herein are new oral pharmaceutical compositions of MGBG and related polyamine analogs, polyamine biosynthesis inhibitors, polyamine inhibitors of AMD-I and regulators of osteopontin, and their application for the treatment of disease.
• METHODS AND COMPOSITIONS FOR TREATMENT OF DEMYELINATING DISEASES
  申请人：PATHOLOGICA LLC

  公开号：US20150359761A1

  公开（公告）日：2015-12-17

  Disclosed herein are new oral pharmaceutical compositions of SAMDC inhibitors, polyamine analogs, and polyamine biosynthesis inhibitors, and their application for the treatment of conditions including demyelinating diseases, autoimmune disorders affecting the nervous system, and other neurodegenerative conditions.
• US8258186B2
  申请人：——

  公开号：US8258186B2

  公开（公告）日：2012-09-04
• US9616035B2
  申请人：——

  公开号：US9616035B2

  公开（公告）日：2017-04-11