NRL-1049 is a selective inhibitor of ROCK2, demonstrating an IC50 of 0.59 µM for ROCK2 and 26 µM for ROCK1. This compound effectively reduces Lysophosphatidic acid-induced ROCK activation in endothelial cells and has shown potential in animal models by decreasing lesion volume and hemorrhagic transformation associated with cavernous angiomas. Additionally, NRL-1049 preserves the blood-brain barrier, suppresses seizure activity following brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice, making it a valuable tool for research into neurological disorders and vascular pathologies.
NRL-1049 is a selective inhibitor of ROCK2, demonstrating an IC50 of 0.59 µM for ROCK2 and 26 µM for ROCK1. This compound effectively reduces Lysophosphatidic acid-induced ROCK activation in endothelial cells and has shown potential in animal models by decreasing lesion volume and hemorrhagic transformation associated with cavernous angiomas. Additionally, NRL-1049 preserves the blood-brain barrier, suppresses seizure activity following brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice, making it a valuable tool for research into neurological disorders and vascular pathologies.
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