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Hydroxyfasudil(HA-1100)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Hydroxyfasudil(HA-1100)图片
CAS NO:105628-72-6
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)307.37
FormulaC14H17N3O3S
CAS No.155558-32-0 (HCl salt); 105628-72-6 (free)
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 68 mg/mL (197.8 mM)
Water: 68 mg/mL (197.8 mM)
Ethanol: <1 mg/mL
SMILES O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O
Synonyms HA-1100; HA 1100; HA1100; HA-1100 HCl
实验参考方法
In Vitro

In vitro activity: Fasudil (1-10 μM) and hydroxyfasudil (0.3-10 μM) significantly prevented endothelin-induced cardiomyocyte hypertrophy. 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.


Kinase Assay: Hydroxyfasudil HCl (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. It acts as a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil prevents the downregulation of endothelial NO synthase (eNOS) under hypoxic conditions. In a concentration-dependent manner, hydroxyfasudil increases eNOS mRNA and protein expression, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L. This correlates with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively.


Cell Assay: Human vascular endothelial cells are treated with increasing concentrations of hydroxyfasudil (0.1 to 100 μmol/L) and eNOS expression and activity are measured.

In VivoIntracoronary administration of hydroxyfasudil(HF) causes a significant coronary vasodilation of both small arteries and arterioles in a dose-dependent manner under control conditions with a resultant increase in CBF(coronary blood flow). Intracoronary hydroxyfasudil does not significantly alter mean aortic pressure or heart rate. Pretreatment with hydroxyfasudil markedly reduces the I/R-induced myocardial infarct size, and this beneficial effect of hydroxyfasudil is significantly attenuated by L-NMMA. NO may be involved in those cardiovascular protective effects of hydroxyfasudil. Hydroxyfasudil may also be effective for the treatment of pulmonary hypertension. HF protects the myocardium subjected to pacing-induced ischaemia through the increase in the regional myocardial blood flow.
Animal modelMongrel dogs
Formulation & DosageDissolved in saline; 10, 30, and 100 μg/kg; Intracoronary administration
ReferencesStroke. 2005 Oct;36(10):2251-7; J Am Coll Cardiol. 2005 Feb 15;45(4):599-607; Br J Pharmacol. 2001 Dec;134(8):1724-30.