AS-1892802

AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC₅₀s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).¹ It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC₅₀ values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED₅₀ = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.^2,3

WARNING This product is not for human or veterinary use.

1. Yoshimi, E., Kumakura, F., Hatori, C., et al. Antinociceptive effects of AS1892802, a novel Rho kinase inhibitor, in rat models of inflammatory and noninflammatory arthritis. J. Pharmacol. Exp. Ther. 334(3), 955-963 (2010).

2. Yoshimi, E., Yamamoto, H., Furuichi, Y., et al. Sustained analgesic effect of the Rho kinase inhibitor AS1892802 in rat models of chronic pain. J. Pharmacobiodyn 114(1), 119-122 (2010).

3. Takeshita, N., Yoshimi, E., Hatoria, C., et al. Alleviating effects of AS1892802, a Rho kinase inhibitor, on osteoarthritic disorders in rodents. J. Pharmacol. Sci. 115(4), 481-489 (2011).