2-Bromo-N-[11-(2-bromo-acetylamino)-undecyl]-acetamide | 6580-72-9

• 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-[11-(2-bromo-acetylamino)-undecyl]-acetamide
• 英文别名: 2-bromo-N-[11-[(2-bromoacetyl)amino]undecyl]acetamide
• CAS: 6580-72-9
• 化学式: C₁₅H₂₈Br₂N₂O₂
• 分子量: 428.208
• InChiKey: VXTCIULNDJVKET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  21
• 可旋转键数：
  14
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.87
• 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 、 1,11-十一烷二胺 在 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 2.0h， 以56%的产率得到2-Bromo-N-[11-(2-bromo-acetylamino)-undecyl]-acetamide
  参考文献：
  名称：

  [EN] PEPTIDE CONJUGATES AND METHODS OF USE
  [FR] CONJUGUÉS PEPTIDIQUES ET MÉTHODES D'UTILISATION

  摘要：

  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。

  公开号：

  WO2021113535A1

文献信息

• [EN] LONG-ACTING DUAL GIP/GLP-1 PEPTIDE CONJUGATES AND METHODS OF USE<br/>[FR] CONJUGUÉS PEPTIDIQUES DOUBLE GIP/GLP-1 À ACTION PROLONGÉE ET PROCÉDÉS D'UTILISATION
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2022257979A1

  公开（公告）日：2022-12-15

  Provided herein are peptides and peptide conjugates comprising a dual glucose-dependent insulinotropic polypeptide (GIP) and GLP-1 receptor agonist. The peptides may be used for blood glucose management and treating conditions such as diabetes, obesity, non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH).

  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。
• 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.
• [EN] GLP2 RECEPTOR AGONISTS AND METHODS OF USE<br/>[FR] AGONISTES DU RÉCEPTEUR GLP2 ET MÉTHODES D'UTILISATION
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2021113524A2

  公开（公告）日：2021-06-10

  Peptide conjugates comprising a peptide that modulates the GLP-2 receptor are provided. The peptide conjugates may be used for treating conditions responsive to modulation of the GLP-2 receptor. Further provided are stapled GLP-2 peptide conjugates.