AS 1892802 is a potent, ATP-competitive ROCK inhibitor with IC50 values of 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively. In rat models, AS 1892802 has been shown to prevent the formation of tibial cartilage lesions due to MIA induction of osteoarthritis.
R. Li et al. Fragment-Based and Structure-Guided Discovery and Optimization of Rho Kinase Inhibitors. J. Med. Chem. 2012, 55, 2474−2478.
N. Takeshita et al. Alleviating Effects of AS1892802, a Rho Kinase Inhibitor, on Osteoarthritic Disorders in Rodents. J. Pharmacol. Sci. 2011, 115, 481–489.
E. Yoshimi et al. Antinociceptive effects of AS1892802, a novel Rho kinase inhibitor, in rat models of inflammatory and noninflammatory arthritis. J. Pharmacol. Exp. Ther. 2010, 334, 955-963.
E. Yoshimi et al. Sustained analgesic effect of the Rho kinase inhibitor AS1892802 in rat models of chronic pain. J. Pharmacol. Sci. 2010, 114, 119-122.