The applicant provides a compound for enhancing the space coupling degree of an endothelial cell ion channel complex TRPV4- KCa2.3 and anti-hypertension applications thereof. By finding the structural domains of the interacting sites of the endothelial cell ion channel complex TRPV4-KCa2.3, a compound with specificity which can act at the two interacting sites is prepared in the present invention. It is found that the compound can enhance the space coupling degree of the TRPV4-KCa2.3 complex and has great significance for the research and development of anti-hypertension drugs.