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Merck
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Key Documents

H139

Sigma-Aldrich

HA-1077 dihydrochloride

solid, ≥98% (HPLC)

Sinonimo/i:

1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride

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About This Item

Formula empirica (notazione di Hill):
C14H17N3O2S · 2HCl
Numero CAS:
Peso molecolare:
364.29
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

solid

Condizioni di stoccaggio

desiccated

Colore

white to off-white

Solubilità

H2O: >10 mg/mL

Stringa SMILE

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
NOXXIYDYFSNHDF-UHFFFAOYSA-N

Applicazioni

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)

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

Eyeshields, Gloves, type N95 (US)


Certificati d'analisi (COA)

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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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