Preclinical Development
Several preclinical efficacy and safety studies
have been conducted with SLx-3XXX.
Efficacy
SLx-3XXX has been identified as a potent, highly selective inhibitor of ROCK-II in vitro, The compound inhibits stress fiber formation, cellular migration, and endothelial cell tube formation in vitro, and inhibits angiogenesis in Matrigel® plug assays in vivo, establishing its activity as a ROCK2 inhibitor in cells and in vivo.
In preclinical studies, SLx-3XXX has demonstrated efficacy in inflammatory, fibrotic models.
In the UUO model, treatment with SLx-3XXX resulted in a marked decrease in macrophage infiltration, fibronectin and TNFa expression.
SLx-3XXX
series are ROCK 2 selective molecules that are being
optimized for activity against diseases
characterized by inflammation and fibrosis. |