产品描述:
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).{40426} 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.{40427,40428}