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Hydroxyfasudil

CAS No. : 105628-72-6

MCE 站：Hydroxyfasudil

产品活性：Hydroxyfasudil 是一种 ROCK 抑制剂，可抑制 ROCK1 和 ROCK2 的活性，IC₅₀ 值分别为 0.73 和 0.72 μM。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad

作用靶点：ROCK

In Vitro: Hydroxyfasudil is a ROCK inhibitor, with IC₅₀s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC₅₀ of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC₅₀ value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM.

In Vivo: Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  TGF-beta/Smad Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Anti-COVID-19 Compound Library  |  NMPA-Approved Drug Library  |  Cytoskeleton Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Y-27632 dihydrochloride  |  Chroman 1  |  Fasudil Hydrochloride  |  Narciclasine  |  Ripasudil  |  GSK429286A  |  Y-33075  |  CMPD101  |  H-1152 dihydrochloride  |  BDP5290  |  SR-3677  |  SB-772077B dihydrochloride  |  Hydroxyfasudil hydrochloride  |  Pentanoic acid  |  ZINC00881524  |  Verosudil  |  ROCK-IN-1  |  ROCK2-IN-2

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