14-[2-[2-[2-[2-[2-[2-[[(1S)-1-carboxy-4-oxopentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-14-oxotetradecanoic acid

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 14-[2-[2-[2-[2-[2-[2-[[(1S)-1-carboxy-4-oxopentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-14-oxotetradecanoic acid
• 化学式: C₃₂H₅₇N₃O₁₂
• 分子量: 675.8
• InChiKey: DGAXPIGMPFYCIH-MHZLTWQESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  47
• 可旋转键数：
  34
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  216
• 氢给体数：
  5
• 氢受体数：
  12

文献信息

• DOUBLE-ACYLATED GLP-1 DERIVATIVES
  申请人：Novo Nordisk A/S

  公开号：US20140088005A1

  公开（公告）日：2014-03-27

  The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K 27 , and the second K residue is designated K T ; which derivative comprises two albumin binding moieties attached to K 27 and K T , respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC—(CH 2 ) x —CO— and HOOC—C 6 H 4 -0-(CH 2 ) y —CO—; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula —NH—(CH 2 ) 2 —(O—(CH 2 ) 2 ) k —O—(CH 2 ) n —CO—, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or ester thereof. The invention also relates to the pharmaceutical use thereof, for example in the treatment and/or prevention of all forms of diabetes and related diseases, as well as to corresponding novel GLP-1 analogues. The derivatives are suitable for oral administration.