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Merck

H139

Sigma-Aldrich

HA-1077 dihydrochloride

solid, ≥98% (HPLC)

Synonym(e):

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

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About This Item

Empirische Formel (Hill-System):
C14H17N3O2S · 2HCl
CAS-Nummer:
Molekulargewicht:
364.29
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

solid

Lagerbedingungen

desiccated

Farbe

white to off-white

Löslichkeit

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

InChIKey

NOXXIYDYFSNHDF-UHFFFAOYSA-N

Anwendung

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. Wirkung

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.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

Eyeshields, Gloves, type N95 (US)


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Fasudil exerts cardioprotection in Animal Models of Myocardial Ischemia/Reperfusion injury: A Meta-analysis and Review of Preclinical Evidence and Possible Mechanisms
Huang Y, et al.
Frontiers in Pharmacology, 9, 1083-1083 (2018)
M Seto et al.
European journal of pharmacology, 195(2), 267-272 (1991-03-26)
We examined the effects of HA1077, a potent inhibitor of protein kinases in vitro, on the relationship between tension and myosin-light chain (MLC20) phosphorylation in the initial phase of contraction of the rabbit aorta. The dose-response curve of HA1077 for
The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells
Negoro N, et al.
Biochemical and Biophysical Research Communications, 262(1), 211-215 (1999)
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
Manar Hamed Arafa et al.
Life sciences, 254, 117605-117605 (2020-04-13)
Although chloroquine and diclofenac are not cardiovascular drugs, their chronic administration may trigger cardiotoxicity. We, therefore, evaluated the cardiotoxic impact of diclofenac in chloroquine-treated adjuvant arthritic rats and the protective role of Rho-kinase inhibitors. 90 male rats were equally distributed

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