氨基-PEG36-羧酸 盐酸盐

• 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
• 中文名称: 氨基-PEG36-羧酸 盐酸盐
• 英文名称: amino-PEG₃₆-acid
• 英文别名: Amino-PEG36-acid；3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
• 化学式: C₇₅H₁₅₁NO₃₈
• 分子量: 1675.01
• InChiKey: QKMSNDXWGWBERW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -8.8
• 重原子数：
  114
• 可旋转键数：
  110
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.99
• 拓扑面积：
  396
• 氢给体数：
  2
• 氢受体数：
  39

反应信息

• 作为反应物：
  描述：

  炔丙基-PEG5-NHS酯 、 氨基-PEG36-羧酸 盐酸盐 在 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 propargyl-(PEG₅)(PEG₃₆)-acid
  参考文献：
  名称：

  [EN] INSULIN DIMER-INCRETIN CONJUGATES
  [FR] CONJUGUÉS DIMÈRES D'INSULINE-INCRÉTINE

  摘要：

  已披露将胰岛素二聚体与至少具有一种胰岛素增效活性的肽共轭化。

  公开号：

  WO2017189342A1

文献信息

• [EN] INSULIN-INCRETIN CONJUGATES<br/>[FR] CONJUGUÉS D'INSULINE-INCRÉTINE
  申请人：MERCK SHARP & DOHME

  公开号：WO2017160669A1

  公开（公告）日：2017-09-21

  Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.

  胰岛素-胰高血糖素共轭物包括具有在胰高血糖素样1（GLP-1）受体、胰高血糖素（GCG）受体和/或胃抑制性蛋白（GIP）受体上激动剂活性的肽与具有在胰岛素受体上激动剂活性的胰岛素分子结合，以及利用这些共轭物治疗代谢性疾病，例如2型糖尿病。
• MODIFIED RELAXIN POLYPEPTIDES COMPRISING A PHARMACOKINETIC ENHANCER AND USES THEREOF
  申请人：Bristol-Myers Squibb Company

  公开号：US20180222960A1

  公开（公告）日：2018-08-09

  The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

  本公开涉及改良的Relaxin多肽，例如改良的人类Relaxin 2多肽，包括与药代增强剂相连的非自然编码氨基酸，并且这些多肽的治疗用途，例如用于治疗心血管疾病（如心力衰竭）和/或与纤维化相关的疾病。
• Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US10266578B2

  公开（公告）日：2019-04-23

  The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

  本公开一般涉及改良的松弛素多肽，如改良的人松弛素 2 多肽，包括与药代动力学增强剂相连的非天然编码氨基酸，以及此类多肽的治疗用途，如用于治疗心血管疾病（如心力衰竭）和/或与纤维化有关的疾病。
• Antibody peptide conjugates that have agonist activity at both the glucagon and glucagon-like peptide 1 receptors
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10800826B2

  公开（公告）日：2020-10-13

  Described are antibody peptide conjugates (APCs) comprising an antibody conjugated to a peptide analog of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have agonist activity at the glucagon (GCG) receptor and the glucagon-like peptide 1 (GLP-1) receptor and the use of such APCs for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.

  所述抗体多肽共轭物（APCs）包括与胰高血糖素多肽类似物共轭的抗体、经改良后可抗二肽基肽酶 IV（DPP-IV）的裂解和失活，并可延长肽类似物的体内半衰期，同时使肽类似物在胰高血糖素（GCG）受体和胰高血糖素样肽 1（GLP-1）受体上具有激动剂活性、非酒精性脂肪肝（NAFLD）、非酒精性脂肪性肝炎（NASH）和肥胖症等代谢性疾病。
• Method of treating cardiovascular disease and heart failure with modified relaxin polypeptides
  申请人：BRISTOL-MYERS SQUIBB COMPANY

  公开号：US11185570B2

  公开（公告）日：2021-11-30

  The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

  本公开一般涉及改良的松弛素多肽，如改良的人松弛素 2 多肽，包括与药代动力学增强剂相连的非天然编码氨基酸，以及此类多肽的治疗用途，如用于治疗心血管疾病（如心力衰竭）和/或与纤维化有关的疾病。