Fmoc-Cys(Trt) | 1286651-36-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: Fmoc-Cys(Trt)
• 英文别名: 9H-fluoren-9-ylmethyl N-[(2R)-3-oxo-1-tritylsulfanylbutan-2-yl]carbamate
• CAS: 1286651-36-2
• 化学式: C₃₈H₃₃NO₃S
• 分子量: 583.751
• InChiKey: JEYBBMGPRVTFMJ-BHVANESWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.2
• 重原子数：
  43
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  80.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Fmoc-Gly-Wang resin 、 炔丙基脲 、 Fmoc-L-亮氨酸 、 Fmoc-Cys(Trt) 、 N-(9-fluorenylmethoxycarbonyl)-2,2,4,6,7-pentamethyl-2H-benzofuran-5-sulfonyl-L-arginine 、 Fmoc-O-叔丁基-L-酪氨酸 在 哌啶 、 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 作用下， 以 N-甲基吡咯烷酮 为溶剂， 生成
  参考文献：
  名称：

  A water soluble CuI–NHC for CuAAC ligation of unprotected peptides under open air conditions

  摘要：

  据报道，一种不含还原剂的 CuAAC 可在露天条件下工作。CuIâNHC 易于合成、亲水性强且高度稳定，可在毫摩尔浓度下对含有敏感侧链的无保护肽进行清洁连接。

  DOI：

  10.1039/c2cc30515a

文献信息

• Design, synthesis and biological activity of new neurohypophyseal hormones analogues conformationally restricted in the N-terminal part of the molecule. Highly potent OT receptor antagonists
  作者：Anna Kwiatkowska、Monika Ptach、Lenka Borovičková、Jiřina Slaninová、Bernard Lammek、Adam Prahl

  DOI：10.1007/s00726-011-1109-6

  日期：2012.8

  In this study we present the synthesis and some pharmacological properties of fourteen new analogues of neurohypophyseal hormones conformationally restricted in the N-terminal part of the molecule. All new peptides were substituted at position 2 with cis-1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc). Moreover, one of the new analogues: [cis-Apc2, Val4]AVP was also prepared in N-acylated forms

  在这项研究中，我们介绍了 14 种新的神经垂体激素类似物的合成和一些药理学特性，这些类似物在分子的N端部分构象受到限制。所有新肽在 2 位被顺式-1-氨基-4-苯基环己烷-1-羧酸（顺式-Apc）取代。此外，一种新的类似物：[ cis -Apc 2 , Val 4 ]AVP 也制备成具有各种庞大酰基的N-酰化形式。测试了所有肽的升压、抗利尿和体外子宫收缩活性。我们还确定了所选化合物对人 OT 受体的结合亲和力。我们的结果表明，引入顺式 -装甲运兵2中任一或AVP OT的位置2上导致具有高效力antioxytocin类似物。两种新化合物 [Mpa 1 , cis -Apc 2 ]AVP 和 [Mpa 1 , cis -Apc 2 ,Val 4 ]AVP 是非常有效的抗子宫收缩剂（分别为 pA 2  = 8.46 和 8.40）并表现出更高的亲和力对于人类 OT 受体，比阿托西班 ( K i值
• Vitamin-targeted imaging agents
  申请人：Leamon P. Christopher

  公开号：US20070031334A1

  公开（公告）日：2007-02-08

  The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid of the formula H 2 NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
• VITAMIN-TARGETED IMAGING AGENTS
  申请人：LEAMON Christopher P.

  公开号：US20090324499A1

  公开（公告）日：2009-12-31

  The invention relates to compounds and methods for targeting radionuclide-based imaging agents to cells having receptors for a vitamin, or vitamin receptor binding derivative or analog thereof, by using such a vitamin as the targeting ligand for the imaging agent. The invention provides a compound of the formula for use in such methods. In the compound, V is a vitamin that is a substrate for receptor-mediated transmembrane transport in vivo, or a vitamin receptor binding derivative or analog thereof, L is a divalent linker, R is a side chain of an amino acid of the formula H 2 NCHRCOOH, M is a cation of a radionuclide, n is 1 or 0, K is 1 or 0, and the compound can be in a pharmaceutically acceptable carrier therefor. The vitamin-based compounds can be used to target radionuclides to cells, such as a variety of tumor cell types, for use in diagnostic imaging of the targeted cells.
• EX VIVO FLOW CYTOMETRY METHOD AND DEVICE
  申请人：Low Philip Stewart

  公开号：US20100055735A1

  公开（公告）日：2010-03-04

  The invention relates to a method for diagnosing a disease state mediated by pathogenic cells. The method comprises the steps of combining with an ex vivo patient sample a composition comprising a conjugate or complex of the general formula A b -X wherein the group A b comprises a ligand that binds to the pathogenic cells and the group X comprises an imaging agent, and detecting the pathogenic cells that express a receptor for the ligand using flow cytometry.
• PSMA BINDING LIGAND-LINKER CONJUGATES AND METHODS FOR USING
  申请人：PURDUE RESEARCH FOUNDATION

  公开号：US20160151508A1

  公开（公告）日：2016-06-02

  Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical compositions containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.