Fasudil . hydrochloride

Fasudil . Hydrochloride is a potent, cell-permeable, and selective inhibitor of Rho-associated protein kinase (ROCK), with an IC₅₀ of approximately 10.7 µM. It is widely used in research involving vascular biology, neuroprotection, and cytoskeletal dynamics. Fasudil inhibits ROCK-mediated phosphorylation of myosin light chain, leading to smooth muscle relaxation and reduced cellular contractility.

Key features and applications include:

• Selective ROCK Inhibition: Targets ROCK1 and ROCK2, key regulators of actin cytoskeleton and cell motility.
• Neuroprotective Effects: Reduces axonal degeneration and apoptosis in neuronal models; protects against hypoxia-reoxygenation injury.
• Anti-Inflammatory Activity: Inhibits neutrophil transendothelial migration and microglial activation.
• Vascular Relaxation: Used in studies of cerebral vasospasm and pulmonary hypertension due to its vasodilatory effects.
• Bone Regeneration: Promotes osteoblastic differentiation via BMP-2 signaling.

Research Applications:

• Neurodegeneration and stroke models
• Vascular biology and endothelial function
• Inflammation and immune cell migration
• Bone and cartilage tissue engineering
• Cancer cell invasion and metastasis

Relevant disease states include:

• Cerebral Vasospasm: Clinically used in some countries to treat subarachnoid hemorrhage-induced vasospasm.
• Neurodegenerative Diseases: Investigated for its ability to protect neurons in models of ALS, Parkinson’s, and Alzheimer’s disease.
• Pulmonary Hypertension: Explored for its role in reducing vascular resistance and remodeling.
• Osteoporosis and Bone Healing: Enhances osteoblast activity and bone matrix production.
• Cancer: Shown to suppress MMP-2 expression and induce apoptosis in glioblastoma and other tumor models.