Description
A potent ROCK inhibitor (IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively); 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; inhibits PKACα and PRKX (IC50s = 200 and 325 nM, respectively); reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis; has analgesic-like effects in a rat model of streptozotocin-induced diabetic neuropathy; reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis