N2-(1-氧代十四烷基)-L-精氨酸 | 60372-80-7

• 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: N2-(1-氧代十四烷基)-L-精氨酸
• 英文名称: mono-Nα-myristoyl-L-arginine
• 英文别名: N2-(1-Oxotetradecyl)-L-arginine；(2S)-5-(diaminomethylideneamino)-2-(tetradecanoylamino)pentanoic acid
• CAS: 60372-80-7
• 化学式: C₂₀H₄₀N₄O₃
• 分子量: 384.563
• InChiKey: ANKFOZDLPDQNEO-KRWDZBQOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  27
• 可旋转键数：
  18
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  131
• 氢给体数：
  4
• 氢受体数：
  4

安全信息

• 海关编码：
  2925290090

反应信息

• 作为反应物：
  描述：

  N2-(1-氧代十四烷基)-L-精氨酸 、 阿糖胞苷 在 吡啶 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 生成 N-((S)-1-((1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)amino)-5-guanidino-1-oxopentan-2-yl)tetradecanamide
  参考文献：
  名称：

  Synthesis and evaluation of anti-tumor activities of N4 fatty acyl amino acid derivatives of 1-β-arabinofuranosylcytosine

  摘要：

  1-beta-D-Arabinofuranosylcytosine (Ara-C, Cytarabine) is one of the drugs used for acute nonlympbocytic leukemia (ANLL). However, the bioavailability of Ara-C is relatively low due to its low lipophilicity. In order to improve the lipophilicity and bioavailability of Ara-C, a series of N-4 derivatives of Ara-C, i.e., (fatty acid)-(amino acid)-Ara-C analogues, were prepared. The 15 derivatives synthesized were characterized by their melting points, optical rotations and partition coefficients. It was found that the Ara-C derivatives synthesized in this study were more lipophilic than Ara-C as determined by their partition coefficients. Their in vitro cytotoxicity and in vivo anti-tumor activity were determined and compared with that of Ara-C. It was found that the derivatives were more active than Ara-C in Hela cells, but not in HL-60 cells. The in vivo results showed that some of the derivatives were more effective than Ara-C in mice bearing S-180 tumor while others showed a decreased activity in comparison with Ara-C. (C) 2009 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2009.02.028
• 作为产物：
  描述：

  methyl (2S)-5-(diaminomethylideneamino)-2-(tetradecanoylamino)pentanoate 在 sodium hydroxide 作用下， 生成 N2-(1-氧代十四烷基)-L-精氨酸
  参考文献：
  名称：

  Synthesis and evaluation of anti-tumor activities of N4 fatty acyl amino acid derivatives of 1-β-arabinofuranosylcytosine

  摘要：

  1-beta-D-Arabinofuranosylcytosine (Ara-C, Cytarabine) is one of the drugs used for acute nonlympbocytic leukemia (ANLL). However, the bioavailability of Ara-C is relatively low due to its low lipophilicity. In order to improve the lipophilicity and bioavailability of Ara-C, a series of N-4 derivatives of Ara-C, i.e., (fatty acid)-(amino acid)-Ara-C analogues, were prepared. The 15 derivatives synthesized were characterized by their melting points, optical rotations and partition coefficients. It was found that the Ara-C derivatives synthesized in this study were more lipophilic than Ara-C as determined by their partition coefficients. Their in vitro cytotoxicity and in vivo anti-tumor activity were determined and compared with that of Ara-C. It was found that the derivatives were more active than Ara-C in Hela cells, but not in HL-60 cells. The in vivo results showed that some of the derivatives were more effective than Ara-C in mice bearing S-180 tumor while others showed a decreased activity in comparison with Ara-C. (C) 2009 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2009.02.028

文献信息

• [EN] BINDING-SITE MODIFIED LECTINS AND USES THEREOF<br/>[FR] LECTINES DE SITE DE LIAISON MODIFIÉES ET USAGE CORRESPONDANT
  申请人：SMARTCELLS INC

  公开号：WO2010088261A1

  公开（公告）日：2010-08-05

  In one aspect, the disclosure provides cross-linked materials that include multivalent lectins with at least two binding sites for glucose, wherein the lectins include at least one covalently linked affinity ligand which is capable of competing with glucose for binding with at least one of said binding sites; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, wherein the two or more affinity ligands compete with glucose for binding with the lectins at said binding sites and wherein conjugates are cross-linked within the material as a result of non-covalent interactions between lectins and affinity ligands on different conjugates. These materials are designed to release amounts of conjugate in response to desired concentrations of glucose. Depending on the end application, in various embodiments, the conjugates may also include a drug and/or a detectable label.

  在一个方面，该公开提供了包括多价凝集素的交联材料，其中该多价凝集素具有至少两个葡萄糖结合位点，其中该凝集素包括至少一个与亲和配体共价连接的亲和配体，该亲和配体能够与至少一个所述结合位点中的葡萄糖竞争结合；以及包括绑定到共轭框架的两个或更多个独立亲和配体的共轭物，其中这两个或更多个亲和配体与葡萄糖在所述结合位点上与凝集素竞争结合，其中由于不同共轭物上的凝集素和亲和配体之间的非共价相互作用，共轭物在材料内交联。这些材料旨在根据所需葡萄糖浓度释放共轭物的量。根据最终应用，在各种实施例中，共轭物还可以包括药物和/或可检测标记。
• DRUG-LIGAND CONJUGATES, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO
  申请人：Kane John

  公开号：US20130131310A1

  公开（公告）日：2013-05-23

  The present invention relates to methods for synthesizing compounds of formula I or pharmaceutically acceptable salts thereof: (I) wherein each of X, Alk, and W are as defined and described herein.

  本发明涉及一种合成式I化合物或其药用可接受盐的方法：（I），其中X、Alk和W中的每一个如本文所定义和描述。
• Cosmetic composition
  申请人：AJINOMOTO CO., INC.

  公开号：US20030165448A1

  公开（公告）日：2003-09-04

  A cosmetic composition for skin and/or hair, which comprises at least one kind of substance selected from the group consisting of an N &agr; ,N G -di-acylarginine, for example, a compound represented by the following general formula (I): 1 wherein R 1 and R 2 each independently represents a straight or branched-chain alkyl group having 1 to 21 carbon atoms or a straight or branched-chain alkenyl group having 2 to 21 carbon atoms. The cosmetic composition imparts much moistness and superior conditioning effects such as body or elasticity to hair, and to skin, said composition does not impart tackiness and blocked feeling, whilst imparts superior feeling of use such as moistness.

  一种用于皮肤和/或头发的化妆品组合物，其包含以下所述组中选择的至少一种物质，即N&agr;，NG-二酰基精氨酸，例如，由下述一般式（I）表示的化合物：其中R1和R2各自独立地表示具有1至21个碳原子的直链或支链烷基或具有2至21个碳原子的直链或支链烯基。该化妆品组合物为头发提供了很多湿润和优越的调理效果，例如体积或弹性，而对于皮肤，该组合物不会产生黏腻和堵塞感，同时提供了优越的使用感，例如湿润感。
• SYNTHETIC CONJUGATES AND USES THEREOF
  申请人：Zion Todd C.

  公开号：US20110275560A1

  公开（公告）日：2011-11-10

  The present disclosure provides a cross-linked material comprising conjugates which include two or more separate affinity ligands bound to a non-polymeric framework, wherein the molecular weight of the non-polymeric framework is less than 10,000 Da; and multivalent cross-linking agents that non-covalently bind the affinity ligands of the conjugates and thereby cross-link the conjugates to form a cross-linked material, wherein the non-covalent bonds between the multivalent cross-linking agents and the affinity ligands are competitively dissociated in the presence of excess amounts of a target molecule. The present disclosure also provides methods of making and methods of using these materials. In other aspects, the present disclosure provides exemplary conjugates including conjugates for use in glucose responsive cross-linked materials.

  本公开提供一种交联材料，包括共轭物，其包括绑定于非聚合框架上的两个或更多个独立亲和配体，其中非聚合框架的分子量小于10,000 Da；以及多价交联剂，其非共价地结合共轭物的亲和配体，从而交联共轭物形成交联材料，其中多价交联剂与亲和配体之间的非共价键在存在过量的目标分子时被竞争性解离。本公开还提供制备这些材料的方法和使用这些材料的方法。在其他方面，本公开提供了示例共轭物，包括用于葡萄糖响应性交联材料的共轭物。
• CRYSTALLINE INSULIN-CONJUGATES
  申请人：Zion Todd C.

  公开号：US20110281791A1

  公开（公告）日：2011-11-17

  The present disclosure provides crystalline insulin-conjugates. The present disclosure also provides formulations, methods of treatment, methods of administering, and methods of making that encompass these crystalline insulin-conjugates.

  本公开提供晶体胰岛素共轭物。本公开还提供包括这些晶体胰岛素共轭物的配方、治疗方法、给药方法和制备方法。