Mpa-Har-Gly-Asp-Trp-Pro-Cys-NH2 | 135900-78-6

• 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: Mpa-Har-Gly-Asp-Trp-Pro-Cys-NH2
• 英文别名: deamino-Cys-hArg-Gly-Asp-Trp-Pro-Cys-NH2；(3S)-4-[[(2S)-1-[(2S)-2-[[(2R)-1-amino-1-oxo-3-sulfanylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-[[2-[[(2S)-6-(diaminomethylideneamino)-2-(3-sulfanylpropanoylamino)hexanoyl]amino]acetyl]amino]-4-oxobutanoic acid
• CAS: 135900-78-6
• 化学式: C₃₅H₅₁N₁₁O₉S₂
• 分子量: 833.99
• InChiKey: BNVXDQCMSQOXSS-LROMGURASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.7
• 重原子数：
  57
• 可旋转键数：
  23
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.51
• 拓扑面积：
  328
• 氢给体数：
  12
• 氢受体数：
  12

反应信息

• 作为反应物：
  描述：

  Mpa-Har-Gly-Asp-Trp-Pro-Cys-NH2 在 ammonium hydroxide 作用下， 以 水 、 乙腈 为溶剂， 反应 2.0h， 以63%的产率得到依替巴肽
  参考文献：
  名称：

  Novel diphenylmethyl-Derived Amide Protecting Group for Efficient Liquid-Phase Peptide Synthesis: AJIPHASE

  摘要：

  An efficient method for the synthesis of peptides bearing an amide at the C-terminal is described. This method involves the attachment of a C-terminal protecting group bearing long aliphatic chains, followed by the repetition of simple reaction and precipitation steps with the combined advantages of liquid-phase peptide synthesis (LPPS) and solid-phase peptide synthesis (SPPS). Using this method, a hydrophobic peptide was successfully synthesized in good yield and high purity, which cannot be obtained satisfactorily by SPPS.

  DOI：

  10.1021/ol302002g
• 作为产物：
  描述：

  tert-butyl (7S,13S)-13-(((S)-1-((S)-2-(((R)-1-amino-1-oxo-3-(tritylthio)propan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-7-(4-guanidinobutyl)-5,8,11-trioxo-1,1,1-triphenyl-2-thia-6,9,12-triazapentadecan-15-oate 在 三异丙基硅烷 、 1,2-乙二硫醇 、 三氟乙酸 作用下， 反应 2.0h， 生成 Mpa-Har-Gly-Asp-Trp-Pro-Cys-NH2
  参考文献：
  名称：

  Methods for the production of peptide derivatives

  摘要：

  这项发明涉及一种通过固相合成和后组装溶液相合成相结合的方法制备C-末端酰胺衍生物的肽。这些C-末端酰胺衍生物的肽进一步转化为肽醋酸酯。该发明还涉及纯肽醋酸酯和受保护的肽前体。

  公开号：

  US20060276626A1

文献信息

• Active agent delivery sytems and methods for protecting and administering active agents
  申请人：Shire LLC

  公开号：EP2266590A2

  公开（公告）日：2010-12-29

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂给药系统，更具体地说，涉及由与活性剂共价连接的氨基酸（作为单个氨基酸或肽）组成的组合物以及给药共轭活性剂组合物的方法。
• Delivery system and methods for protecting and administering dextroamphetamine
  申请人：Shire LLC

  公开号：EP2316469A1

  公开（公告）日：2011-05-04

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂给药系统，更具体地说，涉及由与活性剂共价连接的氨基酸（作为单个氨基酸或肽）组成的组合物以及给药共轭活性剂组合物的方法。
• Solid phase Fmoc chemistry process to prepare peptides
  申请人：Saksena Lal Divya

  公开号：US20070249806A1

  公开（公告）日：2007-10-25

  The present invention relates to an improved process for the preparation of N 6 -(aminoiminomethyl)-N 2 -(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(16)-disulfide of formula (1), which involves assembling a peptide chain comprising of six amino acids and a thioalkyl carboxylic acid in a required sequence on a solid support to obtain a peptide bound resin of formula (2), capping the free amino groups after each coupling, cleaving Dde group in the peptide of formula (2) from the solid support to obtain peptide-solid support of formula (3), guanylating the peptide of formula (3) at ε-lysine-NH 2 in an organic solvent to obtain peptide-solid support of formula (4), cleaving and deprotecting all groups in the peptide of formula (4) from the solid support to obtain peptide-amide formula (5), oxidizing the SH-peptide of formula (5) with an appropriate oxidizing agent to obtain the crude peptide-amide of formula (1) and purifying the crude peptide-amide of formula (1) by chromatographic technique. The solid support is either resin or a cellulose support like cotton, gauze, fabric, paper and perloza beads. The described process is simple, easy, environment friendly, takes lesser time and more cost effective
• US7897724B2
  申请人：——

  公开号：US7897724B2

  公开（公告）日：2011-03-01
• US9562071B2
  申请人：——

  公开号：US9562071B2

  公开（公告）日：2017-02-07