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].
Hydroxyfasudil HCl/羟基法舒地尔盐酸盐 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bovine aortic endothelial cells (BAEC)
0.1 to 100 μmol/L
48 hours
Did not affect eNOS promoter activity
Stroke. 2005 Oct;36(10):2251-7
Human saphenous vein endothelial cells (HSVEC)
10 μmol/L
18 hours
Increased eNOS mRNA expression to 156±20%
Stroke. 2005 Oct;36(10):2251-7
Human umbilical vein endothelial cells (HUVEC)
10 μmol/L
18 hours
Increased eNOS mRNA expression to 160±10%
Stroke. 2005 Oct;36(10):2251-7
Human aortic endothelial cells (HAEC)
0.1 to 100 μmol/L
18 hours
Increased eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L
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