| AS1892802 is a novel and highly selective Rho kinase (ROCK) inhibitor. AS1892802 potently inhibits human ROCK1 (hROCK1), hROCK2, and rat ROCK2 (rROCK2) with IC50s of 122, 52 and 57 nM, respectively. AS1892802 diminishes the inhibition of CYP isoforms for 3A4, 2D6, 1A2, 2C9, and 2C19 with IC50s of 15, 17, 25, 13, and 19 μM, respectively.[1] AS1892802 inhibits IL-1β–induced PGE2 production in a synovial cell line.[2] Orally administered AS1892802 exhibits potent antinociceptive effect in an adjuvant-induced arthritis (AIA) model (inflammatory arthritis model). Orally administered AS1892802 exhibits potent antinociceptive effect in a monoiodoacetate-induced arthritis (MIA) model (noninflammatory arthritis model), with an ED50 of 0.15 mg/kg (MIA model).[1] |
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