6-methyl-5-oxoheptanethioic S-acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 6-methyl-5-oxoheptanethioic S-acid
• 化学式: C₈H₁₄O₂S
• 分子量: 174.26
• InChiKey: IRCYYGAKFWXVAJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  11
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  35.1
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• BIOLOGICALLY ACTIVE COMPOUND CONJUGATED TO A STAPLED OR STITCHED PEPTIDE
  申请人：Sutura Therapeutics Ltd

  公开号：US20200353092A1

  公开（公告）日：2020-11-12

  The invention relates to improvements in drug delivery and more particularly to the use of Cell Penetrating Agents (CPA's) or Cell Penetrating Peptides (CPP's) which have been stabilized by, for example: i) stapling two amino acids to form Stapled CPP's (StaP's) or ii) stitching three or more amino acids to form stitched CPP's (StiP's). These stabilized CPP's are conjugated to a drug or Biologically Active Compound (BAC) directly or via a Bi-Functional Linker (BFL) so that the BAC can be carried though a cell membrane by the CPP. The resulting molecules are referred to as Drug Carrying Cell Penetrating Molecules (DCCPM's). The preferred BAC is an electrically low charge carrying oligonucleotide such as a phosphorodiamidate morpholino oligonucleotide (PMO). The invention also relates to a method of facilitating the uptake of a BAC into a cell, the use of a DCCPM in the treatment of a disease requiring alteration of an endogenous or exogenous gene, a method of improving the bioavailability of a drug or BAC, a method of introducing a drug or BAC to a site which is refractory to the drug or BAC in its native state, a method of treating a subject comprising administering the DCCPM's of the invention and to a pharmaceutical composition comprising the DCCPM and one or more pharmaceutically acceptable excipients.