替考拉宁

• 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
• 中文名称: 替考拉宁
• 英文名称: (1S,2R,19R,22R,34S,37R,40R,52R)-2-[(2R,3R,4R,5S,6R)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-22-azaniumyl-5,15-dichloro-64-[(2S,3R,4R,5S,6R)-3-(decanoylamino)-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-26,31,44,49-tetrahydroxy-21,35,38,54,56,59-hexaoxo-47-[(2R,3S,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-7,13,28-trioxa-20,36,39,53,55,58-hexazaundecacyclo[38.14.2.23,6.214,17.219,34.18,12.123,27.129,33.141,45.010,37.046,51]hexahexaconta-3,5,8,10,12(64),14,16,23(61),24,26,29(60),30,32,41(57),42,44,46(51),47,49,62,65-henicosaene-52-carboxylate
• 化学式: C88H97Cl2N9O33
• 分子量: 1879.7
• InChiKey: BJNLLBUOHPVGFT-QRZIFLFXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  132
• 可旋转键数：
  20
• 环数：
  16.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  662
• 氢给体数：
  24
• 氢受体数：
  34

反应信息

• 作为反应物：
  描述：

  替考拉宁 、 、 、 、 水 在 (1S,2R,19R,22R,34S,37R,40R,52S)-2,64-bis[[(2R,3S,4R,5S,6S)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy]-22-amino-5,15-dichloro-26,31,44,49-tetrahydroxy-21,35,38,54,56,59-hexaoxo-47-[(2R,3S,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-7,13,28-trioxa-20,36,39,53,55,58-hexazaundecacyclo[38.14.2.23,6.214,17.219,34.18,12.123,27.129,33.141,45.010,37.046,51]hexahexaconta-3,5,8,10,12(64),14,16,23(61),24,26,29(60),30,32,41(57),42,44,46(51),47,49,62,65-henicosaene-52-carboxylic acid 作用下， 以 盐酸 、 六氟异丙醇 为溶剂， 反应 20.0h， 以as obtained by fermentation of strain ATCC 31121 according to U.S的产率得到(1S,2R,19R,22R,34S,37R,40R,52S)-2,64-bis[[(2R,3S,4R,5S,6S)-3-acetamido-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy]-22-amino-5,15-dichloro-26,31,44,49-tetrahydroxy-21,35,38,54,56,59-hexaoxo-47-[(2R,3S,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-7,13,28-trioxa-20,36,39,53,55,58-hexazaundecacyclo[38.14.2.23,6.214,17.219,34.18,12.123,27.129,33.141,45.010,37.046,51]hexahexaconta-3,5,8,10,12(64),14,16,23(61),24,26,29(60),30,32,41(57),42,44,46(51),47,49,62,65-henicosaene-52-carboxylic acid
  参考文献：
  名称：

  Chemical process for preparing L 17392 (deglucoteicoplanin) and its salts

  摘要：

  本发明涉及一种化学过程，用于制备抗生素L 17392（去葡糖基替考普兰）及其与碱和酸的盐，通过将替考普兰化合物或类似替考普兰化合物提交给受控制的强酸性水解条件。

  公开号：

  US04629781A1

文献信息

• ANTI-WALL TEICHOIC ANTIBODIES AND CONJUGATES
  申请人：GENENTECH, INC.

  公开号：US20150366985A1

  公开（公告）日：2015-12-24

  The invention provides anti-wall teichoic acid antibodies and antibiotic conjugates thereof, and methods of using the same.

  这项发明提供了抗壁母细胞酸抗体及其抗生素结合物，以及使用它们的方法。
• SKIN PERMEABLE PEPTIDE AND METHOD FOR USING SAME
  申请人：IUCF-HYU (Industry-University Cooperation Foundation Hanyang University)

  公开号：EP3336098A1

  公开（公告）日：2018-06-20

  The present disclosure is directed to providing a new skin-penetrating peptide, a fusion product with a biologically active substance bound using the same, a cosmetic composition containing the same and a pharmaceutical composition for external application to skin containing the same. The skin-penetrating peptide of the present disclosure is less likely to cause an immune response as compared to existing skin-penetrating peptides and exhibits remarkably improved skin permeability. Therefore, the biologically active substance can be effectively delivered through the skin, particularly through the stratum corneum.

  本公开旨在提供一种新的皮肤穿透肽、使用该肽与生物活性物质结合的融合产品、含有该肽的化妆品组合物以及含有该肽的用于皮肤外用的药物组合物。与现有的皮肤穿透肽相比，本公开的皮肤穿透肽引起免疫反应的可能性更小，而且皮肤渗透性显著提高。因此，生物活性物质可以有效地通过皮肤，特别是角质层输送。
• Skin-penetrating peptide and method for using same
  申请人：IUCF-HYU (INDUSTRY-UNIVERSITY COOPERATION FOUNDATION HANYANG UNIVERSITY)

  公开号：US10858395B2

  公开（公告）日：2020-12-08

  The present disclosure is directed to providing a new skin-penetrating peptide, a fusion product with a biologically active substance bound using the same, a cosmetic composition containing the same and a pharmaceutical composition for external application to skin containing the same. The skin-penetrating peptide of the present disclosure is less likely to cause an immune response as compared to existing skin-penetrating peptides and exhibits remarkably improved skin permeability. Therefore, the biologically active substance can be effectively delivered through the skin, particularly through the stratum corneum.

  本公开旨在提供一种新的皮肤穿透肽、使用该肽与生物活性物质结合的融合产品、含有该肽的化妆品组合物以及含有该肽的用于皮肤外用的药物组合物。与现有的皮肤穿透肽相比，本公开的皮肤穿透肽引起免疫反应的可能性更小，而且皮肤渗透性显著提高。因此，生物活性物质可以有效地通过皮肤，特别是角质层输送。
• SKIN PERMEATING AND CELL ENTERING (SPACE) PEPTIDES AND METHODS OF USE THEREOF
  申请人：The Regents of the University of California

  公开号：US20140161871A1

  公开（公告）日：2014-06-12

  The present disclosure provides peptides and peptide compositions, which facilitate the delivery of an active agent or an active agent carrier wherein the compositions are capable of penetrating the stratum corneum (SC) and/or the cellular membranes of viable cells.
• SKIN PERMEATING AND CELL ENTERING (SPACE) PEPTIDES AND METHODS OF USE THEREFOR
  申请人：CONVOY THERAPEUTICS

  公开号：US20140227174A1

  公开（公告）日：2014-08-14

  Compositions that facilitate the delivery of an active agent or an active agent carrier wherein the compositions are capable of penetrating the stratum corneum (SC) and/or the cellular membranes of viable cells are provided. In some embodiments, the compositions include a peptide, an active agent, and a carrier that includes the active agent, wherein the peptide has an amino acid sequence set forth in any of SEQ ID NOs: 1-18; the peptide is associated with and/or conjugated to the active agent, the carrier, or both; the carrier is selected from the group consisting of a micelle, a liposome, an ethosome, and combinations thereof; and the composition is capable of penetrating a stratum corneum (SC) layer when contacted therewith or penetrating a cell when contacted therewith, and optionally wherein the composition further includes one or more free peptides having an amino acid sequence set forth in any of SEQ ID NOs: 1-18. Also provided are methods for delivering active agents to subjects, methods for treating subjects having dermatological diseases, and methods for attenuating expression of mRNAs of subjects in need thereof and/or for treating diseases and/or disorders thereby.