| CAS NO: | 105628-72-6 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 307.37 |
| Cas No. | 105628-72-6 |
| Formula | C14H17N3O3S |
| Synonyms | HA-1100;HA 1100;HA1100 |
| Solubility | Soluble in DMSO |
| Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one |
| Canonical SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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):338‐340.
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):1136‐1143.
4. Saito M, Ohmasa F, Dimitriadis F, et al. Hydroxyfasudil ameliorates penile dysfunction in the male spontaneously hypertensive rat. Pharmacol Res. 2012;66(4):325‐331.
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):679‐683.
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