The invention relates to a conjugate or a pharmaceutically acceptable salt thereof, the conjugate being of formula: C-L-A, wherein C is a chelator, L is a linker covalently bound to the chelator and A is a Gastrin-releasing peptide receptor antagonist covalently bound to the linker, characterized in that:
- the chelator is of formula:
where the dotted line represents the covalent bond to the linker;
- the linker is of formula: -β-Ala-β-Ala-; and
- the Gastrin-releasing peptide receptor antagonist has the amino acid sequence: -DPhe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2.
The invention also relates to the uses of the conjugate or salt thereof.
本发明涉及一种共轭物或其药学上可接受的盐,该共轭物的结构式为C-L-A,其中 C 是
螯合剂,L 是与
螯合剂共价结合的连接体,A 是与连接体共价结合的胃泌素释放肽受体拮抗剂,其特征在于:
-
螯合剂为式
其中虚线表示与连接体的共价键;
- 连接体为式-β-Ala-β-Ala-;以及
- 胃泌素释放肽受体拮抗剂的
氨基酸序列为-DPhe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2。
本发明还涉及共轭物或其盐的用途。