L(Nle)AQ | 1610618-54-6

• 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: L(Nle)AQ
• 英文别名: (2S)-2-[(3S)-3-methyl-4-[(2S)-2-[(3S)-3-(2-methylpropyl)-2-oxopiperazin-1-yl]hexanoyl]-2-oxopiperazin-1-yl]pentanediamide
• CAS: 1610618-54-6
• 化学式: C₂₄H₄₂N₆O₅
• 分子量: 494.635
• InChiKey: WRTHYDNQBKGXRB-VJANTYMQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  35
• 可旋转键数：
  12
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  159
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2-[(2S,5R,8S,11S)-5-Benzyl-11-[3-(diaminomethylideneamino)propyl]-8-[4-[[4-(3-methoxy-3-oxopropyl)sulfanyl-4-oxobutanoyl]amino]butyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid 、 Fmoc-L-亮氨酸 、 Fmoc-L-丙氨酸 、 、 2-溴乙醇 生成 L(Nle)AQ
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• Oxopiperazine helix mimetics for control of Hypoxia-Inducible gene expression
  申请人：NEW YORK UNIVERSITY

  公开号：US10787424B2

  公开（公告）日：2020-09-29

  The present invention relates to oxopiperazines that mimic helix αB of the C-terminal transactivation domain of HIF1α. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).

  本发明涉及可模拟 HIF1α C 端转录激活结构域的螺旋 αB 的氧哌嗪类化合物。本发明还公开了含有这些氧化哌嗪的药物组合物和使用这些氧化哌嗪的方法（例如，减少基因转录、治疗或预防由 HIF1a 与 CREB 结合蛋白和/或 p300 的相互作用介导的疾病、减少或预防组织中的血管生成、诱导细胞凋亡以及减少细胞存活和/或增殖）。
• OXOPIPERAZINE HELIX MIMETICS FOR CONTROL OF HYPOXIA-INDUCIBLE GENE EXPRESSION
  申请人：ARORA Paramjit S.

  公开号：US20170190673A1

  公开（公告）日：2017-07-06

  The present invention relates to oxopiperazines that mimic helix αB of the C-terminal transactivation domain of HIF1α. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1a with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
• [EN] OXOPIPERAZINE HELIX MIMETICS FOR CONTROL OF HYPOXIA-INDUCIBLE GENE EXPRESSION<br/>[FR] MIMÉTIQUES D'HÉLICE D'OXOPIPÉRAZINE POUR LE CONTRÔLE DE L'EXPRESSION GÉNÉTIQUE INDUCTIBLE PAR HYPOXIE
  申请人：UNIV NEW YORK

  公开号：WO2015179547A2

  公开（公告）日：2015-11-26

  The present invention relates to oxopiperazines that mimic helix αB of the C-terminal transactivation domain of HIF1α. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIFla with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).