H-Gly-NHPh(p-Ac) | 148627-62-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: H-Gly-NHPh(p-Ac)
• 英文别名: glycine-(4-acetyl-anilide)；4-Glycylamino-acetophenon；Glycin-(4-acetyl-anilid)；N-(4-acetylphenyl)-2-aminoacetamide
• CAS: 148627-62-7
• 化学式: C₁₀H₁₂N₂O₂
• mdl: MFCD09724258
• 分子量: 192.217
• InChiKey: LOVVDWAISSOSRE-UHFFFAOYSA-N

物化性质

• 沸点：
  431.5±30.0 °C(Predicted)
• 密度：
  1.218±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  72.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  BOC-L-苯丙氨酸 、 H-Gly-NHPh(p-Ac) 在 α-chymotrypsin 作用下， 以 水 为溶剂， 以27.5%的产率得到Boc-Phe-Gly-NHPh(p-Ac)
  参考文献：
  名称：

  Thermodynamics of enzymic synthesis of solid-phase peptides

  摘要：

  The Gibbs free energy changes of the individual and net synthetic equilibrium of solid-phase tert-butyloxycarbonyl-Phe-Gly p-substituted anilides are calculated from the HPLC analysis data for the equilibrium concentrations. A linear free energy relationship is observed for the net synthetic equilibrium and precipitation equilibrium, suggesting that the latter provides the driving force for the chymotryptic synthesis of these insoluble peptides. This conclusion is strongly supported by a linear correlation between the synthetic yield and the square root of the product solubility.

  DOI：

  10.1016/s0040-4020(01)80374-4
• 作为产物：
  描述：

  N-(4-乙酰基苯)-2-氯乙酰胺 在 氨 作用下， 生成 H-Gly-NHPh(p-Ac)
  参考文献：
  名称：

  DE75915

  摘要：

  公开号：

文献信息

• Growth Hormone Conjugate with Increased Stability
  申请人：Johansen Nils Langeland

  公开号：US20110263501A1

  公开（公告）日：2011-10-27

  Novel growth hormone conjugates comprising a growth hormone compound (GH) and a growth hormone binding protein (GHBP) are disclosed. The invention also encompasses a novel derivatization method for producing stable, long-lasting conjugate (hGH-GHBP) by site specific conjugation. The novel GH-GHBP conjugates have an extended half-life in circulation that facilitates therapeutic use of the protein. The GH-GHBP conjugates exhibit pharmacological properties such as increased functional in vivo half-life, improved renal filtration, improved protease protection and albumin binding.

  揭示了包括生长激素化合物（GH）和生长激素结合蛋白（GHBP）的新型生长激素共轭物。该发明还涵盖了一种用于通过位点特异性结合制备稳定、持久的共轭物（hGH-GHBP）的新型衍生化方法。新型GH-GHBP共轭物在循环中具有延长的半衰期，有助于蛋白质的治疗应用。GH-GHBP共轭物表现出诸如增加的体内功能半衰期、改善的肾脏过滤、改善的蛋白酶保护和结合白蛋白等药理特性。
• Cyclopentapeptide derivatives and uses thereof
  申请人：Technische Universität München

  公开号：EP2380596A1

  公开（公告）日：2011-10-26

  The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.

  本发明涉及具有以下结构的化合物或其药学上可接受的盐，其中Xaa1到Xaa4分别是可选的N-烷基化天然或非天然氨基酸，R是H或甲基，L是连接基团，Ar是包含芳香基团的间隔基团，D包括，优选地是i）有机络合剂和可检测标记的组合；或ii）可检测标记，有机络合剂或活性物质，其中所述活性物质特别被选自细胞毒素、脂质、糖、糖偶联物、糖衍生物、蛋白质和它们的组合，但须注意-L-Ar-D不包括18F-苯甲酰残基。
• Transglutaminase mediated conjugation of peptides
  申请人：Johansen Langeland Nils

  公开号：US20070105770A1

  公开（公告）日：2007-05-10

  Methods for conjugating peptides are provided comprising i) reacting a peptide with a first compound comprising a functional group in the presence of a transglutaminase capable of incorporating said compound into the peptide to form a transaminated peptide, and ii) reacting said transaminated peptide with e.g. a functionalized polymer capable of reacting with the functional group incorporated in the peptide in the enzymatic reaction.

  提供了肽共轭的方法，包括：i)在转谷氨酰胺酶的存在下，将肽与含有官能基的第一化合物反应，使该化合物被并入肽中，形成转氨基化肽；ii)将所述转氨基化肽与具有官能基的聚合物反应，使其与在酶催化反应中并入肽中的官能基发生反应。
• Transglutaminase Mediated Conjugation of Peptides
  申请人：Johansen Nils Langeland

  公开号：US20090264366A1

  公开（公告）日：2009-10-22

  Methods for conjugating peptides are provided comprising i) reacting a peptide with a first compound comprising a functional group in the presence of a transglutaminase capable of incorporating said compound into the peptide to form a transaminated peptide, and ii) reacting said transaminated peptide with e.g. a functionalized polymer capable of reacting with the functional group incorporated in the peptide in the enzymatic reaction.

  本文提供了肽共轭的方法，包括：i）在转酰胺酶存在下，将肽与第一化合物反应，该化合物包含一个官能团，能够将该化合物并入肽中形成转酰胺肽；ii）将转酰胺肽与具有官能团的聚合物反应，该聚合物能够与在酶反应中并入肽中的官能团反应。
• TRANSGLUTAMINASE MEDIATED CONJUGATION OF PEPTIDES
  申请人：NOVO NORDISK A/S

  公开号：EP1708755A2

  公开（公告）日：2006-10-11