cyclo-Arg-Gly-Asp-d-Tyr-Lys | 1169517-62-7

• 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
• 英文名称: cyclo-Arg-Gly-Asp-d-Tyr-Lys
• 英文别名: cRGDyK；cyclo[Arg-Gly-Asp-Tyr-Lys]；2-[(2S,5S,8S,11S)-8-(4-aminobutyl)-11-[3-(diaminomethylideneamino)propyl]-5-[(4-hydroxyphenyl)methyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid
• CAS: 1169517-62-7
• 化学式: C₂₇H₄₁N₉O₈
• 分子量: 619.678
• InChiKey: LAROZEWEPNAWMD-MUGJNUQGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -5
• 重原子数：
  44
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  293
• 氢给体数：
  10
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  cyclo-Arg-Gly-Asp-d-Tyr-Lys 在 氯胺 、 sodium iodide 作用下， 以 水 为溶剂， 反应 0.5h， 以44.7%的产率得到
  参考文献：
  名称：

  [EN] METHODS FOR THE IODINATION OF BIOMOLECULES
  [FR] PROCÉDÉS D'IODATION DE BIOMOLÉCULES

  摘要：

  本文提供了一种碘化生物分子的方法，包括蛋白质和肽。这些方法可以在相对温和的反应条件下成功高效地碘化生物分子。因此，本文描述的方法可用于碘化包括氧化不稳定基团（例如光学染料）在内的生物分子，而不会对氧化不稳定基团产生不利影响。

  公开号：

  WO2018085375A1

文献信息

• A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids
  作者：Pu Zhang、Rongqiang Zhuang、Zhide Guo、Xinhui Su、Xiaoyuan Chen、Xianzhong Zhang

  DOI：10.1002/chem.201604105

  日期：2016.11.14

  A convenient and quantitative radioiodination method by copper‐mediated cross‐coupling of aryl boronic acids was developed. The mild labeling conditions, ready availability of the boronic acid substrate, simple operation, broad functional group tolerance and excellent radiochemical yield (RCY) make this a practical strategy for radioiodine labeling without further purification.

  通过铜介导的芳基硼酸交叉偶联，开发了一种方便，定量的放射性碘化方法。温和的标记条件，易于使用的硼酸底物，简单的操作，宽泛的官能团耐受性和出色的放射化学收率（RCY）使该方法成为无需进一步纯化即可进行放射性碘标记的实用策略。
• Water-soluble Zn–Ag–In–Se quantum dots with bright and widely tunable emission for biomedical optical imaging
  作者：Jie Wang、Rong Zhang、Fangjian Bao、Zhihao Han、Yueqing Gu、Dawei Deng

  DOI：10.1039/c5ra17046j

  日期：——

  In this work, we synthesized water-soluble quaternary cadmium-free Zn–Ag–In–Se quantum dots with bright and widely tunable emission, and explored their potential in tumor-specific imaging in vitro and in vivo.

  在这项工作中，我们合成了水溶性四元无镉Zn-Ag-In-Se量子点，具有明亮且广泛可调的发射，并探索了它们在体外和体内肿瘤特异性成像中的潜力。
• Gadolinium Complex of ¹²⁵I/¹²⁷I-RGD-DOTA Conjugate as a Tumor-Targeting SPECT/MR Bimodal Imaging Probe
  作者：Ji-Ae Park、Jung Young Kim、Yong Jin Lee、Wonho Lee、Sang Moo Lim、Tae-Jeong Kim、Jeongsoo Yoo、Yongmin Chang、Kyeong Min Kim

  DOI：10.1021/ml3003499

  日期：2013.2.14

  The work describes the synthesis and in vivo application of [Gd(L)(H2O)]center dot xH(2)O, where L is a (I-125/I-127-RGD)- DOTA conjugate, as a tumor-targeting SPECT/MR bimodal imaging probe. Here, (I-125/I-127-RGD)-DOTA signifies a "cocktail mixture" of radioisotopic (1a, L = I-125-RGD-DOTA) and natural (1b, L = I-127-RGD-DOTA) Gd complexes. The two complexes are chemically equivalent as revealed by HPLC, and their cocktail mixture exhibits the integrin-specific tumor enhancement, demonstrating that they constitute essentially a single bimodal imaging probe. Employment of a cocktail mixture thus proves to be a sole and practical approach to overcome the sensitivity difference problem between MRI and SPECT.
• [EN] METHODS FOR THE IODINATION OF BIOMOLECULES<br/>[FR] PROCÉDÉS D'IODATION DE BIOMOLÉCULES
  申请人：OHIO STATE INNOVATION FOUNDATION

  公开号：WO2018085375A1

  公开（公告）日：2018-05-11

  Provided herein are methods for iodinating biomolecules, including proteins and peptides. The methods can be used to successfully and efficiently iodinate biomolecules under relatively mild reaction conditions. As a consequence, the methods described herein can be used to iodinate biomolecules that include, for example, an oxidatively unstable moiety (e.g., an optical dye) without adversely impacting the oxidatively unstable moiety.

  本文提供了一种碘化生物分子的方法，包括蛋白质和肽。这些方法可以在相对温和的反应条件下成功高效地碘化生物分子。因此，本文描述的方法可用于碘化包括氧化不稳定基团（例如光学染料）在内的生物分子，而不会对氧化不稳定基团产生不利影响。