(R)-4-(5-(4-methoxybenzamido)pentanamido)octanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 肽模拟物
• 英文名称: (R)-4-(5-(4-methoxybenzamido)pentanamido)octanoic acid
• 英文别名: (4R)-4-[5-[(4-methoxybenzoyl)amino]pentanoylamino]octanoic acid
• 化学式: C₂₁H₃₂N₂O₅
• 分子量: 392.495
• InChiKey: HHBQYKUVBQDSBG-QGZVFWFLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  28
• 可旋转键数：
  14
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  105
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5-氨基颉草酸 在 水 、 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 、 sodium hydroxide 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 生成 (R)-4-(5-(4-methoxybenzamido)pentanamido)octanoic acid
  参考文献：
  名称：

  Inhibitors of secreted phospholipase A 2 suppress the release of PGE 2 in renal mesangial cells

  摘要：

  The upregulation of PGE(2) by mesangial cells has been observed under chronic inflammation condition. In the present work, renal mesangial cells were stimulated to trigger a huge increase of PGE(2) synthesis and were treated in the absence or presence of known PLA(2) inhibitors. A variety of synthetic inhibitors, mainly developed in our labs, which are known to selectively inhibit each of GIVA cPLA(2), GVIA iPLA(2), and GIIA/GV sPLA(2), were used as tools in this study. Synthetic sPLA(2) inhibitors, such as GK115 (an amide derivative based on the non-natural amino acid (R)-gamma-norleucine) as well as GK126 and GK241 (2-oxoamides based on the natural (S)-alpha-amino acid leucine and valine, respectively) presented an interesting effect on the suppression of PGE(2) formation. (C) 2016 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2016.05.017

文献信息

• Inhibitors of secreted phospholipase A 2 suppress the release of PGE 2 in renal mesangial cells
  作者：Sofia Vasilakaki、Efrosini Barbayianni、Victoria Magrioti、Oleksandr Pastukhov、Violetta Constantinou-Kokotou、Andrea Huwiler、George Kokotos

  DOI：10.1016/j.bmc.2016.05.017

  日期：2016.7

  The upregulation of PGE(2) by mesangial cells has been observed under chronic inflammation condition. In the present work, renal mesangial cells were stimulated to trigger a huge increase of PGE(2) synthesis and were treated in the absence or presence of known PLA(2) inhibitors. A variety of synthetic inhibitors, mainly developed in our labs, which are known to selectively inhibit each of GIVA cPLA(2), GVIA iPLA(2), and GIIA/GV sPLA(2), were used as tools in this study. Synthetic sPLA(2) inhibitors, such as GK115 (an amide derivative based on the non-natural amino acid (R)-gamma-norleucine) as well as GK126 and GK241 (2-oxoamides based on the natural (S)-alpha-amino acid leucine and valine, respectively) presented an interesting effect on the suppression of PGE(2) formation. (C) 2016 Elsevier Ltd. All rights reserved.