OW1 is a novel imperatorin derivative that exhibits vasodilative activity. In the present study the antihypertensive effect and inhibition effect on vascular remodeling of OW1 were investigated in 2K1C renovascular hypertensive rats. OW1‐induced vasodilatation in rat mesenteric arteries and renal arteries was evaluated in vitro. 2K1C renovascular hypertensive rats were developed and treated with OW1 (40 and 80 mg/kg/day) for 8 weeks. Blood pressure of rats was measured in conscious. Concentration of microalbumin (mALB) and total protein (U‐TP) of urine and the levels of angiotensin II (Ang II), calcitonin gene‐related peptide (CGRP), and angiotensin‐converting enzyme 1 (ACE) of plasma were detected. The unclipped kidney was stained with hematoxylin and eosin (H&E) and Masson trichrome. The sectioned aortas were stained with Masson trichrome. Immunohistochemical analysis was used to quantify the collagen I and III. OW1 relaxed the rat mesenteric and renal arterial rings in vitro. Treatment of 2K1C hypertensive rats with OW1 (40 and 80 mg/kg/day) for 8 weeks significantly decreased blood pressure Besides, OW1 reduced the Ang II and ACE concentration and raised the CGRP concentration in rat plasma. High doses of OW1 decreased the levels of blood urea nitrogen, mALB and U‐TP. Histology results demonstrated that OW1 reduced renal arteriolar thickness and relieved the structural hypertrophic arteries. Moreover, OW1 caused an inhibition effect on vascular remodeling and renal lesions in hypertensive rats. In summary, the results suggested that OW1 could be a potential novel candidate for hypertension intervention. This article is protected by copyright. All rights reserved.