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Angiotensin Ⅱ (Ang Ⅱ) activates Rho-kinase and initiates the contractile activity in vascular smooth muscle.In this study, we investigated the vasorelaxing effect of DL0805, a Rho-kinase inhibitor, on Ang Ⅱ-induced vascular contractions and its molecular mechanism of action.We found that DL0805 inhibited Ang Ⅱ-induced vascular contractions in both endothelium-intact and endothelium-denuded rat aortic tings.Furthermore, increased phosphorylation level of myosin light chain 2 (MLC2) at Ser19 by Ang Ⅱ stimulation was significantly attenuated by DL0805 in both endothelium-intact and-denuded rat aortic rings.Moreover, DL0805 significantly suppressed Ang Ⅱ-induced Ca2 + influx in VSMCs.In addition, DL0805 was found to block the increase in ERK1/2 phosphorylation at Thr202/Tyr204 in response to Ang Ⅱ in both rat aortic rings and VSMCs.These results demonstrate that DL0805 inhibits Ang Ⅱ-induced rat aortic rings contraction and the mechanism involves the inhibition of Ang Ⅱ-induced Ca2+ influx and ERK1/2 activation.