Hydroxyfasudil hydrochloride acts as a ROCK inhibitor with IC50 values of 0.73 μM for ROCK1 and 0.72 μM for ROCK2. It inhibits PKA less potently, with an IC50 of 37 μM, which is 50 times higher than those for ROCKs. Hydroxyfasudil raises eNOS mRNA levels, exhibiting an EC50 of 0.8 ± 0.3 μM. It also enhances eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC) in a concentration-dependent manner across 0-100 μM. At a concentration of 10 μM, Hydroxyfasudil prolongs the half-life of eNOS mRNA from 13 to 16 hours, without influencing eNOS promoter activity within the range of 0.1 to 100 μM [1].
体外研究
Hydroxyfasudil hydrochloride acts as a ROCK inhibitor with IC50 values of 0.73 μM for ROCK1 and 0.72 μM for ROCK2. It inhibits PKA less potently, with an IC50 of 37 μM, which is 50 times higher than those for ROCKs. Hydroxyfasudil raises eNOS mRNA levels, exhibiting an EC50 of 0.8 ± 0.3 μM. It also enhances eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC) in a concentration-dependent manner across 0-100 μM. At a concentration of 10 μM, Hydroxyfasudil prolongs the half-life of eNOS mRNA from 13 to 16 hours, without influencing eNOS promoter activity within the range of 0.1 to 100 μM [1].
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