5-Benzylhydrogen-N-Boc-Glu-N-hydroxysuccinimidester | 82067-51-4

• 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: 5-Benzylhydrogen-N-Boc-Glu-N-hydroxysuccinimidester
• 英文别名: N^α-Boc-Glu(γ-CH2-C6H5)-OSu；Boc-Glu(-OCH2Ph)-OSu；Boc-Glu(-CH2Ph)-OSu；5-O-benzyl 1-O-(2,5-dioxopyrrolidin-1-yl) 2-[(2-methylpropan-2-yl)oxycarbonylamino]pentanedioate
• CAS: 82067-51-4
• 化学式: C₂₁H₂₆N₂O₈
• 分子量: 434.446
• InChiKey: XVJBCWSNHLGDLQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  31
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  128
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  5-Benzylhydrogen-N-Boc-Glu-N-hydroxysuccinimidester 、 L-天冬氨酸-4-苄酯 以quant.的产率得到N-tert-butyloxycarbonyl(γ-benzyl)glutamyl(β-benzyl)aspartate
  参考文献：
  名称：

  Tetrapetide revealing geroprotective effect, pharmacological substance on its basis, and the method of its application

  摘要：

  提议将L-丙氨酸-L-谷氨酰-L-天冬氨酸-甘氨酸四肽（SEQ ID NO：1）的一般公式L-Ala-L-Glu-L-Asp-Gly（SEQ ID NO：1）作为具有延缓衰老作用的生物活性化合物。建议将L-Ala-L-Glu-L-Asp-Gly（SEQ ID NO：1）四肽在医学上用于制备显示延缓衰老作用的物质。提议一种药理物质，其含有效量的L-丙氨酸-L-谷氨酰-L-天冬氨酸-甘氨酸（L-Ala-L-Glu-L-Asp-Gly）（SEQ ID NO：1）或其氨基（乙酸盐，盐酸盐，草酸盐）和羧基（金属盐-钠，钾，钙，锂，锌，镁，以及有机和无机阳离子的盐-铵和三乙基铵）的盐作为其活性基础。该物质建议用于肌肉注射、鼻腔注射、口服和局部应用。关于本发明，预防和/或治疗老化过早的方法涉及向患者预防性和/或治疗性地施用药理物质，剂量为每天0.01至100μg/kg体重，持续一段时间以达到治疗效果。

  公开号：

  US06727227B1

文献信息

• [EN] NEAR-INFRARED FLUORESCENT CONTRAST BIOIMAGING AGENTS AND METHODS OF USE THEREOF<br/>[FR] AGENTS DE CONTRASTE POUR LA BIOIMAGERIE DANS LE PROCHE INFRAROUGE ET LEURS MÉTHODES D'UTILISATION
  申请人：BETH ISRAEL HOSPITAL

  公开号：WO2015066290A1

  公开（公告）日：2015-05-07

  The instant invention provides near-infrared fluorescent biological contrast agents and methods of using them.

  这项发明提供了近红外荧光生物对比剂及其使用方法。
• Molecules for Gene Delivery and Gene Therapy, and Methods of Use Thereof
  申请人：Grinstaff Mark W.

  公开号：US20090221684A1

  公开（公告）日：2009-09-03

  One aspect of the present invention relates to a synthetic non-viral vector composition for gene therapy. Another aspect of the invention relates to the use of the composition for in vitro, ex vivo and/or in vivo transfer of genetic material. The invention also encompasses a pharmaceutical composition (useful for delivery of nucleic acids to a cell), containing a non-cationic amphiphilic molecule or macro-molecule; or a cationic amphiphilic molecule or macromolecule that transforms from a cationic entity to an anionic, neutral, or zwitterionic entity upon a chemical, photochemical, or biological reaction. Another aspect of the invention relates to multicationic compounds that are composed of three or more amino acids. The present invention also relates to the use of the pharmaceutical composition for delivery of nucleic acids to a cell. Moreover, the invention encompasses the non-viral vector compositions tethered to a surface. The surface-tethered compositions are useful for the delivery of nucleic acids to cells in contact with the surface. An additional embodiment of the invention relates to a hydrogel comprising a composition of the invention, and methods of using same for the delivery of genetic material to a cell.

  本发明的一个方面涉及用于基因治疗的合成非病毒载体组合物。另一个方面涉及使用该组合物在体外、体内和/或体外转移遗传物质。该发明还包括一种制药组合物（用于向细胞传递核酸），其中包含非阳离子性的两性分子或大分子；或者是一个阳离子性的两性分子或大分子，在化学、光化学或生物反应中从阳离子实体转变为阴离子、中性或带电离子实体。该发明的另一个方面涉及由三个或更多氨基酸组成的多阳离子化合物。本发明还涉及使用该制药组合物向细胞传递核酸的方法。此外，该发明还涉及附着在表面上的非病毒载体组合物。附着在表面上的组合物可用于将核酸传递到与表面接触的细胞中。该发明的另一个实施例涉及包含本发明组合物的水凝胶，并使用该水凝胶将遗传物质传递给细胞的方法。
• Tetrapetide revealing geroprotective effect, pharmacological substance on its basis, and the method of its application
  申请人：Obschestvo S Ogranichennoi Otvetstven-Nostiju “Klinika Instituta {overscore (B)}ioregulyatsii Gerontologii”

  公开号：US06727227B1

  公开（公告）日：2004-04-27

  Tetrapeptide L-alanyl-L-glutamyl-L-aspartyl-glycine (SEQ ID NO: 1) of the general formula L-Ala-L-Glu-L-Asp-Gly (SEQ ID NO: 1) is proposed as a biologically active compound with a geroprotective effect. The use of L-Ala-L-Glu-L-Asp-Gly (SEQ ID NO: 1) tetrapeptide in medicine is proposed for preparing a substance displaying a geroprotective effect. There is proposed a pharmacological substance, which contains as its active base an effective amount of tetrapeptide of the formula L-alanyl-L-glutamyl-L-aspartyl-glycine (L-Ala-L-Glu-L-Asp-Gly) (SEQ ID NO: 1) or its salts of the amino group (acetate, hydrochloride, oxalate) and of carboxyl groups (the salts of metals-Sodium, Potassium, Calcium, Lithium, Zinc, Magnesium, and also the salts of organic and inorganic cations-ammonium and triethylammonium). The substance is proposed for parenteral, intranasal, oral administration, and local application. With respect to the invention, the method of premature ageing prevention involves prophylactic and/or therapeutic administration to a patient of the pharmacological substance in doses of 0.01 to 100 &mgr;g/kg of the body weight at least once a day for a period necessary for the achievement of a therapeutic effect.

  提议将L-丙氨酸-L-谷氨酰-L-天冬氨酸-甘氨酸四肽（SEQ ID NO：1）的一般公式L-Ala-L-Glu-L-Asp-Gly（SEQ ID NO：1）作为具有延缓衰老作用的生物活性化合物。建议将L-Ala-L-Glu-L-Asp-Gly（SEQ ID NO：1）四肽在医学上用于制备显示延缓衰老作用的物质。提议一种药理物质，其含有效量的L-丙氨酸-L-谷氨酰-L-天冬氨酸-甘氨酸（L-Ala-L-Glu-L-Asp-Gly）（SEQ ID NO：1）或其氨基（乙酸盐，盐酸盐，草酸盐）和羧基（金属盐-钠，钾，钙，锂，锌，镁，以及有机和无机阳离子的盐-铵和三乙基铵）的盐作为其活性基础。该物质建议用于肌肉注射、鼻腔注射、口服和局部应用。关于本发明，预防和/或治疗老化过早的方法涉及向患者预防性和/或治疗性地施用药理物质，剂量为每天0.01至100μg/kg体重，持续一段时间以达到治疗效果。
• Near-infrared fluorescent contrast bioimaging agents and methods of use thereof
  申请人：Beth Israel Deaconess Medical Center

  公开号：US11077210B2

  公开（公告）日：2021-08-03

  The instant invention provides near-infrared fluorescent biological contrast agents and methods of using them.

  本发明提供了近红外荧光生物造影剂及其使用方法。
• NEAR-INFRARED FLUORESCENT CONTRAST BIOIMAGING AGENTS AND METHODS OF USE THEREOF
  申请人：BETH ISRAEL DEACONESS MEDICAL CENTER

  公开号：US20160263249A1

  公开（公告）日：2016-09-15

  The instant invention provides near-infrared fluorescent biological contrast agents and methods of using them.