Hydroxyfasudil hydrochloride
羟基法舒地尔(HA-1100)盐酸
Catalog No.
A3479
Rho激酶抑制剂和血管扩张剂
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Description:
IC50 Value: 0.12 uM (ROCK1); 0.17 uM (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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 343.83 |
Cas No. | 155558-32-0 |
Formula | C14H18ClN3O3S |
Synonyms | HA-1100 hydrochloride;HA 1100 hydrochloride;HA1100 hydrochloride |
Solubility | insoluble in EtOH; ≥7.88 mg/mL in DMSO with gentle warming; ≥5.04 mg/mL in H2O with gentle warming and ultrasonic |
Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one;hydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CNC3=O.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。 |
质量控制和MSDS
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