EMD 527040 hydrochloride is an effective integrin alphaVbeta6 inhibitor. The IC 50 values of EMD 527040 hydrochloride were 6 nM and 1.6 uM to inhibit alphaVbeta6 binding to fibronectin and alphaVbeta6 expression cells to fibronectin, respectively. EMD 527040 hydrochloride shows antifibrotic activity in animal models of biliary fibrosis and is active in vivo.