The invention relates to an application of substituted piperazine-1,4-diamide compounds in pharmacy. The substituted piperazine-1,4-diamide compounds can be used as an activating agent of SIRT1 (Silent Information Regulator 1) for activating nuclear receptors LXRalpha and LXRbeta, regulating expression of target proteins ABCA1/G1, inflammatory key proteins p65, senescence-associated genes p662hc and the like, promoting excretion of lipid and cholesterol, regulating cholesterol metabolism, inflammation-associated and senescence-associated genes or proteins, treating cardiovascular and cerebrovascular diseases, regulating blood lipids and resisting atherosclerosis, inflammatory reaction and senescence diseases.
