(2R)-1-butoxy-3-({8-[(3β)-cholest-5-en-3-yloxy]octyl}oxy)-N,N-dimethylpropan-2-amine | 1266613-79-9

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: (2R)-1-butoxy-3-({8-[(3β)-cholest-5-en-3-yloxy]octyl}oxy)-N,N-dimethylpropan-2-amine
• 英文别名: (2R)-1-butoxy-3-[8-[[(3S,8S,9S,10R,13R,14S,17R)-10,13-dimethyl-17-[(2R)-6-methylheptan-2-yl]-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-yl]oxy]octoxy]-N,N-dimethylpropan-2-amine
• CAS: 1266613-79-9
• 化学式: C₄₄H₈₁NO₃
• 分子量: 672.132
• InChiKey: ZQFVWHHOHCSFIP-ICFOLOKLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  12.7
• 重原子数：
  48
• 可旋转键数：
  23
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  30.9
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• NOVEL CATATONIC LIPIDS WITH VARIOUS HEAD GROUPS FOR OLIGONUCLEOTIDE DELIVERY
  申请人：SIRNA THERAPEUTICS. INC.

  公开号：US20160113874A1

  公开（公告）日：2016-04-28

  The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.

  本发明提供了一种新型阳离子脂质，可以与其他脂质成分（如胆固醇和PEG脂质）结合使用，形成含有siRNA的脂质纳米粒子，以促进细胞摄取和内体逃逸，并在体外和体内靶向mRNA进行靶向RNA干扰。
• LIPID NANOPARTICLE VACCINE ADJUVANTS AND ANTIGEN DELIVERY SYSTEMS
  申请人：MERCK SHARP & DOHME CORP.

  公开号：EP3556353A2

  公开（公告）日：2019-10-23

  The instant invention provides for novel lipid nanoparticle (LNP) formulations, containing cationic lipids, for use as vaccine adjuvants and/or as antigen delivery systems. It is an object of the instant invention to provide LNP formulations that demonstrate enhancements in humoral and/or cellular immunogenicity of vaccine antigens, particularly subunit vaccine antigens, when utilized alone or in combination with immunostimulatory agents (e.g. small molecule or oligonucleotide TLR agonists). The instant invention further identifies physical and chemical properties of the LNP formulations that can be manipulated to enhance antigen efficiency and adjuvant tolerability in vivo.

  本发明提供了含有阳离子脂质的新型脂质纳米粒子（LNP）制剂，可用作疫苗佐剂和/或抗原递送系统。本发明的目的是提供 LNP 制剂，当其单独使用或与免疫刺激剂（如小分子或寡核苷酸 TLR 激动剂）结合使用时，可显示出疫苗抗原，特别是亚单位疫苗抗原的体液和/或细胞免疫原性的增强。本发明进一步确定了 LNP 制剂的物理和化学特性，这些特性可通过操作来提高抗原效率和佐剂在体内的耐受性。
• Lipid nanoparticle vaccine adjuvants and antigen delivery systems
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10821175B2

  公开（公告）日：2020-11-03

  The instant invention provides for novel lipid nanoparticle (LNP) formulations, containing cationic lipids, for use as vaccine adjuvants and/or as antigen delivery systems. It is an object of the instant invention to provide LNP formulations that demonstrate enhancements in humoral and cellular immunogenicity of vaccine antigens, particularly subunit vaccine antigens, when utilized alone or in combination with immunostimulatory agents (e.g. small molecule or oligonucleotide TLR agonists). The instant invention further identifies physical and chemical properties of the LNP formulations that can be manipulated to enhance antigen efficiency and adjuvant tolerability in vivo.

  本发明提供了含有阳离子脂质的新型脂质纳米粒子（LNP）制剂，可用作疫苗佐剂和/或抗原递送系统。本发明的目的是提供 LNP 制剂，当单独使用或与免疫刺激剂（如小分子或寡核苷酸 TLR 激动剂）联合使用时，可显示出疫苗抗原，特别是亚单位疫苗抗原的体液和细胞免疫原性增强。本发明进一步确定了 LNP 制剂的物理和化学特性，这些特性可通过操作来提高抗原效率和佐剂在体内的耐受性。
• US9181295B2
  申请人：——

  公开号：US9181295B2

  公开（公告）日：2015-11-10
• US9642804B2
  申请人：——

  公开号：US9642804B2

  公开（公告）日：2017-05-09