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Hydroxyfasudil

羟基法舒地尔
Catalog No.
A3478
Rho激酶抑制剂和血管扩张剂
组合的产品项目
规格价格库存 数量
10mg
¥ 954.00
Ship with 10-15 days
50mg
¥ 3,818.00
Ship with 10-15 days

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A

背景

Description: IC50 Value: 0.73μM (ROCK1); 0.72μM (ROCK2) [1] Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. in vitro: Fasudil (1-10 μM) and hydroxyfasudil (0.3-10 μM) significantly prevented endothelin-induced cardiomyocyte hypertrophy [2]. Hydroxyfasudil significantly attenuated serotonin (IC)-induced vasoconstriction of SA (-7 +/- 1% vs. 2 +/- 1%, p < 0.01). Coronary I/R significantly impaired coronary vasodilation to acetylcholine after I/R (SA, p < 0.05; and A, p < 0.01 vs. before I/R) and L-NMMA further reduced the vasodilation, whereas hydroxyfasudil completely preserved the responses. in vivo: Treatment with hydroxyfasudil significantly improved bladder intercontraction intervals. Rats treated with hydroxyfasudil also showed a significant reduction of histopathological features associated with cystitis [3]. Twelve-week-old male SHRs were treated with hydroxyfasudil (3 or 10 mg/kg, i.p.) once a day for 6 weeks. Treatment with hydroxyfasudil significantly improved the decreased penile cGMP concentrations, the increased Rho kinase activities, the increased norepinephrine-induced contractions, and the decreased acetylcholine-induced relaxation in a dose-dependent manner [4]. Toxicity: The proportion of patients with good clinical outcome was 74.5% (41/55) in the fasudil group and 61.7% (37/60) in the nimodipine group. There were no serious adverse events reported in the fasudil group [5]. Clinical trial: N/A
References:
1.Rikitake Y, et al. Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection. Stroke. 2005 Oct;36(10):2251-7.

2. Satoh S, Kawasaki K, Ikegaki I, Asano T, Shimokawa H. Evidence of a direct cellular protective effect of Rho-kinase inhibitors on endothelin-induced cardiac myocyte hypertrophy. Biochem Biophys Res Commun. 2012;424(2):338340.

3. Shimizu N, De Velasco MA, Umekawa T, Uemura H, Yoshikawa K. Effects of the Rho kinase inhibitor, hydroxyfasudil, on bladder dysfunction and inflammation in rats with HCl-induced cystitis. Int J Urol. 2013;20(11):11361143.

4. Saito M, Ohmasa F, Dimitriadis F, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012;66(4):325331.

5. Zhao J, Zhou D, Guo J, et al. Efficacy and safety of fasudil in patients with subarachnoid hemorrhage: final results of a randomized trial of fasudil versus nimodipine. Neurol Med Chir (Tokyo). 2011;51(10):679683.

化学属性

StorageStore at -20°C
M.Wt307.37
Cas No.105628-72-6
FormulaC14H17N3O3S
SynonymsHA-1100;HA 1100;HA1100
SolubilitySoluble in DMSO
Chemical Name5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
SDFDownload SDF
Canonical SMILESC1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O
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质量控制

质量控制和MSDS

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化学结构

Hydroxyfasudil