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CAS No. : 155558-32-0
MCE 国际站:Hydroxyfasudil hydrochloride
产品活性:Hydroxyfasudil hydrochloride 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 hydrochloride 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 | FDA-Approved Anticancer Drug Library | Human Metabolite Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Off-patent Drug Library | Membrane Protein-targeted Compound Library | Chroman 1 dihydrochloride | Ripasudil free base | AS1892802 | Hu7691 free base | Sovesudil | AT13148 | CRT0066854 | LX7101 | Y-27632 dihydrochloride | RKI-1447 | HA-100 hydrochloride | WF-536 | Pentanoic acid-d9 | Fasudil dihydrochloride | ROCK-IN-5 | ROCK2-IN-5 | BDP5290 | PF-4950834 | PT-262 | Afuresertib hydrochloride | Belumosudil mesylate | GSK429286A | Y-27632 dihydrochloride (GMP) | H-1152 dihydrochloride | 3-(4-Pyridyl)indole | ROCK inhibitor-2 | ROCK-IN-7 | ZINC00881524
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货号: HY-13911A
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