26.27-Bis-nor-5β-cholestan-24-on | 14949-16-7

• 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: 26.27-Bis-nor-5β-cholestan-24-on
• 英文别名: 24-methyl-5β-cholan-24-one；24-Methyl-5β-cholan-24-on；24-Methyl-5β-cholanon-(24)；(5R)-5-[(5S,8R,9S,10S,13R,14S,17R)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]hexan-2-one
• CAS: 14949-16-7
• 化学式: C₂₅H₄₂O
• 分子量: 358.608
• InChiKey: LMGRIFIYAJHRKP-NMQWMWRVSA-N

物化性质

• 沸点：
  427.3±13.0 °C(Predicted)
• 密度：
  0.961±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  8.1
• 重原子数：
  26
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.96
• 拓扑面积：
  17.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  26.27-Bis-nor-5β-cholestan-24-on 在 chromium(VI) oxide 、 盐酸 、 溶剂黄146 作用下， 生成 Methyl-23nor-5β-cholonat
  参考文献：
  名称：

  Wieland; Schlichting; Jacobi, Hoppe-Seyler's Zeitschrift fur Physiologische Chemie, 1926, vol. 161, p. 80,102

  摘要：

  DOI：
• 作为产物：
  描述：

  24-chloromethyl-5β-cholanone-(24) 在 溶剂黄146 、 锌 作用下， 生成 26.27-Bis-nor-5β-cholestan-24-on
  参考文献：
  名称：

  Hollander; Gallagher, Journal of Biological Chemistry, 1946, vol. 162, p. 549,550

  摘要：

  DOI：

文献信息

• HYALURONIC ACID DERIVATIVE HAVING AMINO ACID AND STERYL GROUP INTRODUCED THEREINTO
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：US20150231268A1

  公开（公告）日：2015-08-20

  The present invention provides a hyaluronic acid derivative containing a disaccharide unit represented by formula (I) or formula (I) and (II), and a complex containing the hyaluronic acid derivative and a drug.

  本发明提供了一种含有由化学式（I）或化学式（I）和（II）表示的二糖单元的透明质酸衍生物，以及含有该透明质酸衍生物和药物的复合物。
• MODIFIED iRNA AGENTS
  申请人：MANOHARAN Muthiah

  公开号：US20100076056A1

  公开（公告）日：2010-03-25

  The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent. The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.

  本发明涉及iRNA剂，其中最好包括一个单体，其中核糖基团已被替换为除核糖以外的基团，并进一步包括一个具有一个或多个连接基团的连接件，其中至少一个连接基团是可切断的连接基团。连接件反过来可以连接到所选的基团，例如，配体，例如，靶向或传递基团，或改变物理性质的基团。可切断的连接基团是足够稳定的连接基团，以便在细胞外定向治疗有益量的iRNA剂（例如，单链或双链iRNA剂），通过可切断的连接基团与靶向剂结合，以靶向细胞，但在进入靶细胞后被切断以释放iRNA剂从靶向剂中。包括这样一个单体可以允许调节iRNA剂的一个性质，将其纳入其中，例如，通过使用非核糖基团作为配体或其他实体（例如，亲脂性基团，例如，胆固醇）的连接点，直接或间接地连接。本发明还涉及制备和使用这种修改的iRNA剂的方法。
• IRNA AGENTS WITH BIOCLEAVABLE TETHERS
  申请人：MANOHARAN Muthiah

  公开号：US20100267941A1

  公开（公告）日：2010-10-21

  The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent.

  本发明涉及iRNA代理，它们包括一个单体，其中核糖基团已被替换为其他核糖基团，进一步包括一个具有一个或多个连接基团的连接体，其中至少一个连接基团是可裂解的连接基团。 连接体反过来可以连接到所选的基团，例如配体，例如靶向或递送基团，或改变物理性质的基团。 可裂解的连接基团足够稳定，使其允许将治疗上有益的iRNA代理（例如单链或双链iRNA代理）通过可裂解的连接基团耦合到靶向剂，以靶向细胞，但进入目标细胞后会裂解以释放iRNA代理。
• iRNA AGENTS WITH BIOCLEAVABLE TETHERS
  申请人：Alnylam Pharmaceuticals, Inc.

  公开号：US20130281685A1

  公开（公告）日：2013-10-24

  The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent.

  本发明涉及iRNA代理，其优选包括一个单体，其中核糖基团已被替换为除核糖以外的基团，进一步包括一个具有一个或多个连接基团的缆绳，其中至少一个连接基团是可切断的连接基团。缆绳反过来可以连接到所选的基团，例如配体，例如定向或递送基团，或改变物理性质的基团。可切断的连接基团是足够稳定的连接基团，使其允许通过可切断的连接基团耦合的iRNA代理（例如单链或双链iRNA代理）针对细胞进行治疗上有益的量的靶向，但在进入目标细胞时被切断以释放iRNA代理从定向代理中。
• iRNA AGENTS WITH BIOCLEAVABLE TETHERS
  申请人：Alnylam Pharmaceuticals, Inc.

  公开号：US20150073133A1

  公开（公告）日：2015-03-12

  The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent.

  本发明涉及iRNA药剂，其中最好包括一个单体，其中核糖基团已被其他核糖以外的基团所取代，该基团还包括一个具有一个或多个连接基团的连接件，其中至少一个连接基团是可断裂的连接基团。连接件可以连接到所选的基团，例如配体，例如靶向或递送基团，或改变物理性质的基团。可断裂的连接基团是足够稳定的连接基团，以在细胞外允许将治疗上有益量的iRNA药剂（例如单链或双链iRNA药剂），通过可断裂的连接基团与靶向剂耦合，以靶向细胞，但在进入靶细胞后被断裂以释放iRNA药剂从靶向剂中。