H139
HA-1077 dihydrochloride
solid, ≥98% (HPLC)
Synonym(s):
1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride
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About This Item
Empirical Formula (Hill Notation):
C14H17N3O2S · 2HCl
CAS Number:
Molecular Weight:
364.29
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Recommended Products
Quality Level
assay
≥98% (HPLC)
form
solid
storage condition
desiccated
color
white to off-white
solubility
H2O: >10 mg/mL
SMILES string
Cl[H].Cl[H].O=S(=O)(N1CCCNCC1)c2cccc3cnccc23
InChI
1S/C14H17N3O2S.2ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;;/h1,3-5,7,11,15H,2,6,8-10H2;2*1H
InChI key
NOXXIYDYFSNHDF-UHFFFAOYSA-N
Application
HA-1077 dihydrochloride has been used:
- to relax cantilevers
- in the functional assessment of isolated coronary arteries
- to investigate the effect of azaindole-1, fasudil on acute hypoxic pulmonary vasoconstriction (HPV)
Biochem/physiol Actions
HA-1077/fasudil, is a Rho kinase inhibitor. This ROCK inhibitor has the ability to increase cognitive deficits in animals, that have Alzheimer′s disease (AD). In humans, fasudil possesses high therapeutic effects against cerebral vasospasm after subarachnoid hemorrhage (SAH). HA-1077 also acts as an inhibitor of protein kinases, like myosin light chain kinase and Rho associated kinase. Hence, it can block myosin phosphorylation.
Novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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T Asano et al.
British journal of pharmacology, 98(4), 1091-1100 (1989-12-01)
The in vitro and in vivo vasorelaxant effects of HA1077, 1-(5-isoquinolinesulphonyl)-homopiperazine HCl, a novel vasodilator were examined. The inhibitory effects of HA1077 on contractile responses to various agonists were examined on strips of rabbit aorta. The concentration-response curves to 5-hydroxytryptamine
Protective effects of the ROCK inhibitor fasudil against cognitive dysfunction following status epilepticus in male rats
Song X, et al.
Journal of Neuroscience Research (2018)
Acute pergolide exposure stiffens engineered valve interstitial cell tissues and reduces contractility in vitro
Capulli A K, et al.
Cardiovascular Pathology : the Official Journal of the Society For Cardiovascular Pathology, 25(4), 316-324 (2016)
Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension
Dahal B K, et al.
European heart journal. Cardiovascular pharmacotherapy, erj01403-erj02009 (2010)
M Shirotani et al.
The Journal of pharmacology and experimental therapeutics, 259(2), 738-744 (1991-11-01)
The effects of a newly developed vasodilator agent, HA1077 [1-(5-isoquinolinesulfonyl)-homopiperazine hydrochloride], were investigated on the proliferation of cultured bovine aortic vascular smooth muscle cells (VSMC). HA1077 (10-100 microM) inhibited both fetal calf serum-induced proliferation and [3H]thymidine incorporation into DNA of
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