1 2-二肉豆蔻酰基-Sn-甘油-3-磷酸酯 | 28874-52-4

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 甘油磷脂
• 中文名称: 1 2-二肉豆蔻酰基-Sn-甘油-3-磷酸酯
• 中文别名: (1aS,8aR,8bS)-8a-羟基-6-甲氧基-1,5-二甲基-8-甲亚基-1,1a,2,8,8a,8b-六氢吖丙烯并[2',3':3,4]吡咯并[1,2-a]吲哚-4,7-二酮；12-二肉豆蔻酰基-Sn-甘油-3-磷酸酯
• 英文名称: L-α-dimyristoylphosphatidic acid
• 英文别名: 1,2-dimyristoyl-sn-glycero-3-phosphate；1,2-dimyristoyl-sn-glycero 3-phosphate；(R)-1,2-bis-myristoyloxy-3-phosphonooxy-propane；(R)-1,2-Bis-myristoyloxy-3-phosphonooxy-propan；1,2-O-dimyristoyl-sn-glycero-3-phosphatidic acid；1,2-dimyristoyl-sn-glycero-3-phosphoric acid；Dimyristoyl-sn-glycerol 3-phosphate；[(2R)-3-phosphonooxy-2-tetradecanoyloxypropyl] tetradecanoate
• CAS: 28874-52-4
• 化学式: C₃₁H₆₁O₈P
• 分子量: 592.794
• InChiKey: OZSITQMWYBNPMW-GDLZYMKVSA-N

物化性质

• 熔点：
  60-61 °C
• 沸点：
  668.6±65.0 °C(Predicted)
• 密度：
  1.034±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  10.8
• 重原子数：
  40
• 可旋转键数：
  32
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.94
• 拓扑面积：
  119
• 氢给体数：
  2
• 氢受体数：
  8

安全信息

• 安全说明：
  S22,S24/25
• WGK Germany：
  3
• 海关编码：
  2931900090

反应信息

• 作为反应物：
  描述：

  1 2-二肉豆蔻酰基-Sn-甘油-3-磷酸酯 在 2,4,6-三异丙基苯磺酰氯 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 三氟乙酸 作用下， 以 吡啶 、 二氯甲烷 、 甲苯 为溶剂， 反应 22.5h， 生成 二肉豆蔻酰磷脂酰胆碱
  参考文献：
  名称：

  Bersch, B.; Starck, J. P.; Milon, A., Bulletin de la Societe Chimique de France, 1993, vol. 130, p. 575 - 583

  摘要：

  DOI：
• 作为产物：
  描述：

  二肉豆蔻酰磷脂酰胆碱 在 sodium acetate 、 sodium dodecyl-sulfate 、 溶剂黄146 、 calcium chloride 作用下， 以 乙醚 为溶剂， 反应 240.0h， 生成 1 2-二肉豆蔻酰基-Sn-甘油-3-磷酸酯
  参考文献：
  名称：

  Phospholipid-nucleoside conjugates. 3. Syntheses and preliminary biological evaluation of 1-.beta.-D-arabinofuranosylcytosine 5'-monophosphate-L-1,2-dipalmitin and selected 1-.beta.-D-arabinofuranosylcytosine 5'-diphosphate-L-1,2-diacylglycerols

  摘要：

  Several new phospholipid-ara-C conjugates have been prepared and tested as prodrugs of the parent ara-C. The new derivative include ara-CMP-L-dipalmitin, ara-CDP-L-distearin, ara-CDP-L dimyristin, ara-CDP-L-diolein, and the radioactively labeled derivative ara-CDP-L-di[1-14C]palmitin. In addition, the unusually stable ara-CMP-L-dipalmitin-N-phosphoryldicyclohexylurea adduct was isolated as a crystalline solid (two diastereomers) in the reaction sequence to prepare ara-CMP-L-dipalmitin. The new prodrugs were solubilized by sonication methods and tested for their antiproliferative activity in vitro against mouse myeloma MPC-11 cells and against L1210 lymphoid leukemia. Such studies demonstrated that the antiproliferative activities of the prodrugs (as determined by ED50) were less that ara-C on a molar basis. In the mouse myeloma cell line some evidence was obtained that the antiproliferative activity was related to the chain length of the fatty acid side chains in the prodrugs. In in vivo studies against L1210 lymphoid leukemia in mice, the prodrugs were shown to be much more effective than ara-C, with the overall efficacy apparently being independent of the length of the fatty acid side chain. Some evidence was obtained in the vivo studies that the ara-CDP-L-dimyristin, which bears the shortest fatty acid side chain, was more toxic at the higher dosages than the longer chain length derivatives.

  DOI：

  10.1021/jm00353a010

文献信息

• FLUORESCENT ANTICANCER PLATINUM DRUGS
  申请人：INVICTUS ONCOLOGY PVT. LTD.

  公开号：US20180312534A1

  公开（公告）日：2018-11-01

  The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to fluorescent platinum based compounds. The disclosure further relates to synthesis of said fluorescent platinum based compounds, nanoparticles and compositions comprising said fluorescent platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by the fluorescence changes between aforesaid platinum based compounds and corresponding free ligands, nanoparticles and compositions.

  本公开涉及纳米技术和癌症治疗领域。具体而言，本公开涉及荧光铂基化合物。该公开进一步涉及合成所述荧光铂基化合物、纳米颗粒和包含所述荧光铂基化合物/纳米颗粒的组合物。该公开还涉及通过上述铂基化合物与相应的游离配体、纳米颗粒和组合物之间的荧光变化来管理癌症的方法。
• Growth Hormone Secretagogue Receptor 1A Ligands
  申请人：Schambye Hans T.

  公开号：US20080300180A1

  公开（公告）日：2008-12-04

  The present invention relates to new growth hormone secretagogue receptor 1A (GHS-R 1A) ligands, and pharmaceutical compositions comprising any of the new GHS-R1 A ligands. The ligands are suitable for a wide range of applications, and thus the present invention also relates to use of the GHS-R1 A ligands according to the present invention in the manufacture of a medicament for the treatment of an individual in need thereof. In another aspect, the present invention relates to a method of treatment of an individual in need thereof, comprising administering to said individual one or more of the GHS-R1A ligands disclosed herein, such as e.g. for treatment of cancer cachexia.

  本发明涉及新型生长激素促分泌素受体1A（GHS-R 1A）配体，以及包含任何此类新型GHS-R1A配体的药物组合物。这些配体适用于广泛的应用范围，因此本发明还涉及根据本发明的GHS-R1A配体在制造用于治疗有此需要的个体的药物中的用途。在另一方面，本发明涉及一种治疗有此需要的个体的方法，包括向该个体施用本文披露的一种或多种GHS-R1A配体，例如用于治疗癌症恶病质。
• [EN] LANGERIN+ CELL TARGETING<br/>[FR] CIBLAGE DE CELLULES DE LANGERINE+
  申请人：MAX PLANCK GESELLSCHAFT

  公开号：WO2019141731A1

  公开（公告）日：2019-07-25

  The present invention relates to the use of a vehicle for specific molecular targeting of Langerin+ cells, wherein the vehicle is capable of specifically binding to a Langerin+ cell, said vehicle comprising (a) at least one carrier and (b) at least one saccharide moiety-based conjugate for a targeted cargo delivery into a Langerin+ cell, as well as pharmaceutical compositions and uses comprising the inventive vehicle.

  本发明涉及使用一种车辆来针对Langerin+细胞进行特定分子靶向，其中该车辆能够特异性地结合到Langerin+细胞，所述车辆包括（a）至少一种载体和（b）至少一种基于糖苷基的共轭物，用于将目标载荷传递到Langerin+细胞内，以及包括该创新车辆的药物组合物和用途。
• Amine Cationic Lipids and Uses Thereof
  申请人：Dicerna Pharmaceuticals, Inc.

  公开号：US20140371293A1

  公开（公告）日：2014-12-18

  The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).

  本发明涉及脂质化合物及其用途。具体而言，这些化合物包括一类具有胺基团的阳离子脂质，例如氨基-胺或氨基-酰胺基团。这些脂质化合物可用于体内或体外传递一个或多个药物（例如，多聚阴离子荷载物或反义荷载物，如RNAi药物）。
• HYDROPHILIC FLUORINATED MOLECULES FOR LIPOSOMAL 19F MRI PROBES WITH UNIQUE MR SIGNATURES
  申请人：TEXAS CHILDREN'S HOSPITAL

  公开号：US20180154025A1

  公开（公告）日：2018-06-07

  Readily available hydrophilic and small organofluorine moieties were condensed via “click chemistry” to generate nonionic hydrophilic fluorinated molecules with unique 19 F MR signatures. These were used to fabricate stable liposome formulations for imaging various tissue types. This approach was tailored to exploit the broad spectrum of organic 19 F molecular species and to generate probes with distinct 19 F MRI signatures for simultaneous assessment of multiple molecular targets within the same target volume.

  通过“点击化学”将易得的亲水性和小的有机氟基团缩合，生成具有独特的19F MR标记的非离子亲水性氟化分子。这些分子被用于制备稳定的脂质体配方，用于成像各种组织类型。这种方法旨在利用有机19F分子种类的广泛谱，生成具有不同19F MRI标记的探针，以同时评估同一目标体积内多个分子靶标。