The present application relates to the technical field of biological
medicine, and discloses a screening and
verification method of a small-molecule inhibitor targeting a specific domain of
sclerostin. The compound provided by the present application is obtained by structural modification, skeleton derivation design and molecular docking screening of a lead small-molecule compound
tetrahydrofolic acid targeting the loop3 domain of
sclerostin. The compound can specifically target and combine with the loop3 domain of
sclerostin, can re-activate the Wnt
signal inhibited by sclerostin, and restore the effect of Wnt
signal in promoting
bone formation. The sclerostin inhibitor containing the compound can inhibit various
muscle-skeletal
system diseases mediated by sclerostin activation, has wide application range and strong targeting property. Based on the characteristics that the compound targets and combines with the loop3 domain of sclerostin but not the loop2 domain, when the compound is used for preparing a
drug for preventing and treating diseases mediated by sclerostin, the risk of cardiovascular diseases caused in the process of using the
drug can be reduced.