1973494-16-4

BA-1049 is a selective ROCK2 inhibitor.

NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59?μM and 26?μM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice[1].

ROCK1: 26 μM (IC₅₀); ROCK2: 0.59 μM (IC₅₀)

[1] Mulder IA, et al. The novel ROCK2 selective inhibitor NRL-1049 preserves the blood-brain barrier after acute injury. J Cereb Blood Flow Metab. 2024 Jun 4:271678X241238845. DOI:10.1177/0271678X241238845