Z-FY(t-Bu)-dmk | 114014-15-2

• 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: Z-FY(t-Bu)-dmk
• 英文别名: Z-Phe-Tyr(tBu)-diazomethylketone；benzyl N-[(2S)-1-[[(2S)-4-diazo-1-[4-[(2-methylpropan-2-yl)oxy]phenyl]-3-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate
• CAS: 114014-15-2
• 化学式: C₃₁H₃₄N₄O₅
• 分子量: 542.635
• InChiKey: CGONKNHDBTYOOC-SVBPBHIXSA-N

物化性质

• 溶解度：
  乙酸乙酯：10mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  40
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  95.7
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Z-FY(t-Bu)-dmk 在 水 、 二甲基二环氧乙烷 作用下， 以 丙酮 为溶剂， 反应 1.5h， 生成 Cbz-Phe-Tyr(OBut)-COCHO
  参考文献：
  名称：

  Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L — comparisons of potency and selectivity profiles with cathepsin B

  摘要：

  We have utilized previously known substrate and inhibitor specificity profiles for the lysosomal cysteine protease, cathepsin L, to design a new series of putative inhibitors of this enzyme, based on di- and tri-peptidyl alpha-keto-beta-aldehydes. Kinetic evaluation of those compounds revealed Z-Phe-Tyr(OBut)-COCHO, with a K-i=0.6 nM, to be the most potent, synthetic reversible inhibitor of cathepsin L reported to date. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00340-1
• 作为产物：
  描述：

  Z-Phe-Tyr(OBut)-OH 在 N-甲基吗啉 作用下， 以 乙醚 为溶剂， 反应 0.25h， 生成 Z-FY(t-Bu)-dmk
  参考文献：
  名称：

  Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L — comparisons of potency and selectivity profiles with cathepsin B

  摘要：

  We have utilized previously known substrate and inhibitor specificity profiles for the lysosomal cysteine protease, cathepsin L, to design a new series of putative inhibitors of this enzyme, based on di- and tri-peptidyl alpha-keto-beta-aldehydes. Kinetic evaluation of those compounds revealed Z-Phe-Tyr(OBut)-COCHO, with a K-i=0.6 nM, to be the most potent, synthetic reversible inhibitor of cathepsin L reported to date. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00340-1

文献信息

• Development of peptidyl α-keto-β-aldehydes as new inhibitors of cathepsin L — comparisons of potency and selectivity profiles with cathepsin B
  作者：John F Lynas、Susan J Hawthorne、Brian Walker

  DOI：10.1016/s0960-894x(00)00340-1

  日期：2000.8

  We have utilized previously known substrate and inhibitor specificity profiles for the lysosomal cysteine protease, cathepsin L, to design a new series of putative inhibitors of this enzyme, based on di- and tri-peptidyl alpha-keto-beta-aldehydes. Kinetic evaluation of those compounds revealed Z-Phe-Tyr(OBut)-COCHO, with a K-i=0.6 nM, to be the most potent, synthetic reversible inhibitor of cathepsin L reported to date. (C) 2000 Elsevier Science Ltd. All rights reserved.