(6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-18-yl 2-(dimethylamino)ethyl(ethyl)carbamate | 1346932-57-7

• 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: (6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-18-yl 2-(dimethylamino)ethyl(ethyl)carbamate
• 英文别名: [(6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-18-yl] N-[2-(dimethylamino)ethyl]-N-ethylcarbamate
• CAS: 1346932-57-7
• 化学式: C₄₄H₈₂N₂O₂
• 分子量: 671.147
• InChiKey: YHSXAYWMBWMOFK-AEXQXJJBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  16.1
• 重原子数：
  48
• 可旋转键数：
  36
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  32.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  heptatriaconta-6,9,28,31-tetraen-19-ol 、 N,N-二甲基-N'-乙基乙二胺 、 氯甲酸三氯甲酯 在 吡啶 作用下， 以 乙醚 为溶剂， 反应 1.5h， 以78%的产率得到(6Z,9Z,28Z,31Z)-heptatriaconta-6,9,28,31-tetraen-18-yl 2-(dimethylamino)ethyl(ethyl)carbamate
  参考文献：
  名称：

  [EN] NOVEL CATIONIC LIPIDS AND METHODS OF USE THEREOF
  [FR] NOUVEAUX LIPIDES CATIONIQUES ET PROCÉDÉS D'UTILISATION DE CEUX-CI

  摘要：

  公开号：

  WO2011141705A8

文献信息

• COMPOSITIONS AND METHODS FOR SILENCING APOLIPOPROTEIN B
  申请人：Heyes James

  公开号：US20130123339A1

  公开（公告）日：2013-05-16

  The present invention provides compositions and methods for the delivery of interfering RNAs such as siRNAs that silence APOB expression in cells such as liver cells. In particular, the nucleic acid-lipid particles provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells such as liver cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of APOB 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.

  本发明提供了一种用于传递干扰RNA（如siRNA）的组合物和方法，用于在细胞中（如肝细胞）沉默APOB表达。具体来说，核酸-脂质颗粒能够有效地封装核酸，并有效地将封装的核酸传递给体内的细胞，如肝细胞。本发明的组合物非常有效，因此可以在相对较低的剂量下有效地降低APOB的表达。此外，与先前已知的技术相比，本发明的组合物和方法毒性较低，并且提供了更大的治疗指数。
• Compositions and methods for silencing apolipoprotein B
  申请人：Heyes James

  公开号：US08865675B2

  公开（公告）日：2014-10-21

  The present invention provides compositions and methods for the delivery of interfering RNAs such as siRNAs that silence APOB expression in cells such as liver cells. In particular, the nucleic acid-lipid particles provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells such as liver cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of APOB 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.

  本发明提供了一种组合物和方法，用于递送干扰RNA（如siRNA）以在细胞中（如肝细胞）沉默APOB表达。特别地，核酸脂质颗粒提供了高效的核酸封装和有效的封装核酸递送到体内的细胞（如肝细胞）。本发明的组合物具有高度的效力，因此可以在相对较低的剂量下有效地抑制APOB。此外，本发明的组合物和方法比先前已知的组合物和方法更少毒性，提供更大的治疗指数。
• NOVEL CATIONIC LIPIDS AND METHODS OF USE THEREOF
  申请人：Heyes James

  公开号：US20130123338A1

  公开（公告）日：2013-05-16

  The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids 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 a specific target protein 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.

  本发明提供了传递治疗剂到细胞的组成物和方法。特别地，包括新颖的阳离子脂质和核酸-脂质颗粒，提供对核酸的高效封装和对封装的核酸在体内的高效传递到细胞。本发明的组成物非常有效，因此可以在相对较低的剂量下有效地降低特定目标蛋白的表达。此外，本发明的组成物和方法与先前已知的组成物和方法相比，毒性更低，提供更大的治疗指数。
• US8865675B2
  申请人：——

  公开号：US8865675B2

  公开（公告）日：2014-10-21
• [EN] COMPOSITIONS AND METHODS FOR SILENCING APOLIPOPROTEIN B<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR RÉDUIRE AU SILENCE L'APOLIPOPROTÉINE B
  申请人：PROTIVA BIOTHERAPEUTICS INC

  公开号：WO2011141703A1

  公开（公告）日：2011-11-17

  The present invention provides compositions and methods for the delivery of interfering RNAs such as siRNAs that silence APOB expression in cells such as liver cells. In particular, the nucleic acid-lipid particles provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells such as liver cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of APOB 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.