2-Bromo-N-[7-(2-bromo-acetylamino)-heptyl]-acetamide | 6580-70-7

• 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: 2-Bromo-N-[7-(2-bromo-acetylamino)-heptyl]-acetamide
• 英文别名: 2-bromo-N-[7-[(2-bromoacetyl)amino]heptyl]acetamide
• CAS: 6580-70-7
• 化学式: C₁₁H₂₀Br₂N₂O₂
• 分子量: 372.1
• InChiKey: AROICEAWFUYKCF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  17
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  溴代乙酸酐 、 1,7-二氨基庚烷 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 以64%的产率得到2-Bromo-N-[7-(2-bromo-acetylamino)-heptyl]-acetamide
  参考文献：
  名称：

  [EN] LONG-ACTING DUAL GIP/GLP-1 PEPTIDE CONJUGATES AND METHODS OF USE
  [FR] CONJUGUÉS PEPTIDIQUES DOUBLE GIP/GLP-1 À ACTION PROLONGÉE ET PROCÉDÉS D'UTILISATION

  摘要：

  本文提供了含有双重葡萄糖依赖性胰岛素促泌肽（GIP）和GLP-1受体激动剂的肽和肽共轭物。这些肽可以用于血糖管理和治疗糖尿病、肥胖症、非酒精性脂肪肝病（NAFLD）和非酒精性脂肪性肝炎（NASH）等疾病。

  公开号：

  WO2022257979A1

文献信息

• [EN] PEPTIDE CONJUGATES AND METHODS OF USE<br/>[FR] CONJUGUÉS PEPTIDIQUES ET MÉTHODES D'UTILISATION
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2021113535A1

  公开（公告）日：2021-06-10

  Peptide conjugates comprising a peptide selected from a peptide that modulates the PYY receptor, a peptide that modulates both the GLP-1 receptor and the GCG receptor, a peptide that modulates both the GLP-1 receptor and the GIP receptor, and a peptide that modulates the GLP-1 receptor; and a staple attached to the peptide at a first amino acid and a second amino acid are disclosed herein. Also provided are peptide conjugates comprising prolactin-releasing peptide. The peptide conjugates may be used for treating conditions such as obesity. Further provided are stapled prolactin-releasing peptide.

  本文披露了包括以下内容的肽共轭物：选择自可调节PYY受体的肽、可调节GLP-1受体和GCG受体的肽、可调节GLP-1受体和GIP受体的肽、以及可调节GLP-1受体的肽；以及连接到肽的稳定剂，在第一个氨基酸和第二个氨基酸处连接。还提供了包括催乳素释放肽的肽共轭物。这些肽共轭物可用于治疗肥胖等疾病。此外，还提供了稳定的催乳素释放肽。
• Modified therapeutic agents, stapled peptide lipid conjugates, and compositions thereof
  申请人：THE CALIFORNIA INSTITUTE FOR BIOMEDICAL RESEARCH

  公开号：US10039809B2

  公开（公告）日：2018-08-07

  Methods and compositions are provided for extending the half-life of a therapeutic agent. A modified therapeutic agent (mTA) comprises a therapeutic agent, a staple, and a half-life extending molecule. The mTAs disclosed herein may be used to treat a disease or a condition in a subject in need thereof.

  提供了延长治疗剂半衰期的方法和组合物。改性治疗剂（mTA）由治疗剂、主食和延长半衰期分子组成。本文公开的 mTA 可用于治疗有需要的受试者的疾病或病症。
• Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity
  作者：Sam Lear、Elsa Pflimlin、Zhihong Zhou、David Huang、Sharon Weng、Van Nguyen-Tran、Sean B. Joseph、Shane Roller、Scott Peterson、Jing Li、Matthew Tremblay、Peter G. Schultz、Weijun Shen

  DOI：10.1021/acs.jmedchem.0c00740

  日期：2020.9.10

  Bariatric surgery results in increased intestinal secretion of hormones GLP-1 and anorexigenic PYY, which is believed to contribute to the clinical efficacy associated with the procedure. This observation raises the question whether combination treatment with gut hormone analogs might recapitulate the efficacy and mitigate the significant risks associated with surgery. Despite PYY demonstrating excellent efficacy and safety profiles with regard to food intake reduction, weight loss, and glucose control in preclinical animal models, PYY-based therapeutic development remains challenging given a low serum stability and half-life for the native peptide. Here, combined peptide stapling and PEG-fatty acid conjugation affords potent PYY analogs with >14 h rat half-lives, which are expected to translate into a human half-life suitable for once-weekly dosing. Excellent efficacy in glucose control, food intake reduction, and weight loss for lead candidate 22 in combination with our previously reported long-acting GLP-1 analog is demonstrated in a diet-induced obesity mouse model.
• MODIFIED THERAPEUTIC AGENTS, STAPLED PEPTIDE LIPID CONJUGATES, AND COMPOSITIONS THEREOF
  申请人：THE CALIFORNIA INSTITUTE FOR BIOMEDICAL RESEARCH

  公开号：US20160317623A1

  公开（公告）日：2016-11-03

  Methods and compositions are provided for extending the half-life of a therapeutic agent. A modified therapeutic agent (mTA) comprises a therapeutic agent, a staple, and a half-life extending molecule. The mTAs disclosed herein may be used to treat a disease or a condition in a subject in need thereof.
• [EN] MODIFIED THERAPEUTIC AGENTS, STAPLED PEPTIDE LIPID CONJUGATES, AND COMPOSITIONS THEREOF<br/>[FR] AGENTS THÉRAPEUTIQUES MODIFIÉS, CONJUGUÉS LIPIDE-PEPTIDE AGRAFÉS, ET COMPOSITIONS LES COMPRENANT
  申请人：CALIFORNIA INST BIOMEDICAL RES

  公开号：WO2015095406A1

  公开（公告）日：2015-06-25

  Methods and compositions are provided for extending the half-life of a therapeutic agent. A modified therapeutic agent (mTA) comprises a therapeutic agent, a staple, and a half-life extending molecule. The mTAs disclosed herein may be used to treat a disease or a condition in a subject in need thereof.