Ac-K(Fam)AKKSRRC(gg)VLL-OH | 1159505-97-1

• 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: Ac-K(Fam)AKKSRRC(gg)VLL-OH
• CAS: 1159505-97-1
• 化学式: C₉₉H₁₅₂N₂₀O₂₀S
• 分子量: 1974.48
• InChiKey: NBRDXOJIMMRRJT-SPPPTTSDSA-N

物化性质

• 密度：
  1.32±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  None
• 重原子数：
  None
• 可旋转键数：
  None
• 环数：
  None
• sp3杂化的碳原子比例：
  None
• 拓扑面积：
  None
• 氢给体数：
  None
• 氢受体数：
  None

反应信息

• 作为产物：
  描述：

  (2E,6E,10E)-1-溴-3,7,11,15-四甲基-2,6,10,14-十六碳四烯 、 N2-acetyl-N6-(3',6'-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9'-xanthene]-5-carbonyl)-L-lysyl-L-alanyl-L-lysyl-L-lysyl-L-seryl-L-arginyl-L-arginyl-L-cysteinyl-L-valyl-L-leucyl-L-leucine 在 zinc diacetate 、 三氟乙酸 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 生成 Ac-K(Fam)AKKSRRC(gg)VLL-OH
  参考文献：
  名称：

  Investigation of the sequence and length dependence for cell-penetrating prenylated peptides

  摘要：

  Cell penetrating peptides are useful delivery tools for introducing molecules of interest into cells. A new class of cell penetrating molecules has been recently reported-cell penetrating, prenylated peptides. In this study a series of such peptides was synthesized to examine the relationship between peptide sequence and level of peptide internalization and to probe their mechanism of internalization. This study revealed that prenylated peptides internalize via a non-endocytotic pathway regardless of sequence. Sequence length and identity was found to play a role in peptide uptake but prenylated sequences as short as two amino acids were found to exhibit significant cell penetrating properties. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.11.026

文献信息

• Discovery of dipiperidines as new antitubercular agents
  作者：Elena Bogatcheva、Colleen Hanrahan、Ping Chen、Jacqueline Gearhart、Katherine Sacksteder、Leo Einck、Carol Nacy、Marina Protopopova

  DOI：10.1016/j.bmcl.2009.10.135

  日期：2010.1

  As part of our ongoing research effort to develop new therapeutics for treatment of tuberculosis (TB), we synthesized a combinatorial library of 10,358 compounds on solid support using a pool-and-split technique and tested the resulting compounds for activity against Mycobacterium tuberculosis. Structure activity relationship (SAR) evaluation identified new compounds with antitubercular activity, including a novel hit series that is structurally unrelated to any existing antitubercular drugs, dipiperidines. Dipiperidine representatives exhibited MIC values as low as 7.8 mu M, the ability to induce promoter Rv0341 activated in response to cell wall biosynthesis inhibition, relatively low nonspecific cellular toxicity in the range of 30-162 mu M, and log P values less than 4. (C) 2009 Elsevier Ltd. All rights reserved.