1-[2,2-bis[(9Z,12Z)-octadeca-9,12-dienyl]-1,3-dioxan-5-yl]-N-methylmethanamine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[2,2-bis[(9Z,12Z)-octadeca-9,12-dienyl]-1,3-dioxan-5-yl]-N-methylmethanamine
• 化学式: C₄₂H₇₇NO₂
• 分子量: 628.1
• InChiKey: YRVWJCMHTAAGPA-QYCRHRGJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  15
• 重原子数：
  45
• 可旋转键数：
  32
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  30.5
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Improved amino lipids and methods for the delivery of nucleic acids
  申请人：Tekmira Pharmaceuticals Corporation

  公开号：EP2743265A1

  公开（公告）日：2014-06-18

  The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipid having the structure below and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

  本发明提供了向细胞输送治疗剂的优良组合物和方法。其中特别包括具有以下结构的新型脂质和核酸-脂质颗粒，它们能有效地封装核酸并在体内将封装的核酸高效地输送到细胞中。本发明的组合物具有很高的效力，因此能以相对较低的剂量有效地敲除特定的靶蛋白。此外，与本领域以前已知的组合物和方法相比，本发明的组合物和方法毒性更低，治疗指数更高。