(S)-1-ethoxy-2-amino-4-methylpentane | 134080-98-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (S)-1-ethoxy-2-amino-4-methylpentane
• 英文别名: (2S)-1-ethoxy-4-methylpentan-2-amine
• CAS: 134080-98-1
• 化学式: C₈H₁₉NO
• 分子量: 145.245
• InChiKey: BGHJPIOXKTYCPD-QMMMGPOBSA-N

物化性质

• 沸点：
  191℃
• 密度：
  0.847
• 闪点：
  59℃

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  10
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-1-ethoxy-2-amino-4-methylpentane 在 N-甲基吗啉 、 盐酸 、 氯甲酸异丁酯 作用下， 以 乙酸乙酯 为溶剂， 反应 20.25h， 生成 N-<(S)-1-ethoxy-4-methyl-2-pentyl>-(S)-histidinamide dihydrochloride
  参考文献：
  名称：

  Gastrin releasing peptide antagonists with improved potency and stability

  摘要：

  Gastrin releasing peptide (GRP) is a 27 amino acid peptide hormone which is homologous to the amphibian peptide bombesin. Two series of novel GRP antagonists were developed by C-terminal modification of N-acetyl-GRP-20-27 amide. Peptide derivatives within each series resist enzymatic degradation in serum and exhibit strong affinity for the GRP receptor. The first series of compounds replaces the Leu26-Met27 region of GRP with an alkyl ether moiety. One member of this series, N-acetyl-GRP-20-25-NH-[(S)-1-ethoxy-4-methyl-2-pentane], specifically blocked radiolabeled GRP binding with an IC50 of 6 nM. In the second series of antagonists the oxygen of the ether moiety is replaced with a methylene group, resulting in GRP antagonists which are equipotent to native GRP in receptor binding assays (IC50 = 2 nM) and are also resistant to proteolytic degradation in vitro. All of the C-terminally modified peptides tested blocked GRP-stimulated mitogenesis in Swiss 3T3 mouse fibroblasts. Representative compounds also blocked GRP-induced elevation of [Ca2+]i in human SCLC cells, and inhibited GRP-independent release of gastrin in vivo.

  DOI：

  10.1021/jm00111a027
• 作为产物：
  描述：

  L-亮氨醇 、 碘乙烷 以 四氢呋喃 、 氯仿 、 异丙醇 为溶剂， 生成 (S)-1-ethoxy-2-amino-4-methylpentane
  参考文献：
  名称：

  Gastrin releasing peptide antagonist

  摘要：

  小细胞肺癌细胞（SCLC）含有胃泌素释放肽（GRP）受体。细胞对GRP的反应是快速生长。我们发现了一组肽衍生物，它们作为GRP拮抗剂通过阻止GRP与其受体的结合，从而抑制对GRP生长促进活性敏感的细胞的生长。

  公开号：

  US05019647A1

文献信息

• Purine derivatives for use as medicament and for use in treating neurodegenerative or neuro-inflammatory disorders
  申请人：COMMISSARIAT À L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES

  公开号：US11472807B2

  公开（公告）日：2022-10-18

  Compound of formula (I) and its addition salts with pharmaceutically acceptable acids, and methods in which an effective amount of the compound or any pharmaceutically acceptable salt thereof is administered (as a medicament) to an individual in need thereof.

  式(I)化合物 及其与药学上可接受的酸的加成盐，以及向有需要的人施用有效量的该化合物或其任何药学上可接受的盐的方法（作为药物）。
• BENZOIMIDAZOLE-CARBOXYLIC ACID AMIDE DERIVATIVES FOR TREATING METABOLIC OR CARDIOVASCULAR DISEASES
  申请人：SANOFI

  公开号：EP2897939B1

  公开（公告）日：2017-02-01
• PURINE DERIVATIVES FOR USE AS MEDICAMENT AND FOR USE IN TREATING NEURODEGENERATIVE OR NEURO-INFLAMMATORY DISORDERS
  申请人：COMMISSARIAT À L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES

  公开号：US20200354364A1

  公开（公告）日：2020-11-12

  Compound of formula (I) and its addition salts with pharmaceutically acceptable acids, and methods in which an effective amount of the compound or any pharmaceutically acceptable salt thereof is administered (as a medicament) to an individual in need thereof.
• US5019647A
  申请人：——

  公开号：US5019647A

  公开（公告）日：1991-05-28
• US9156796B2
  申请人：——

  公开号：US9156796B2

  公开（公告）日：2015-10-13