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Merck

H139

HA-1077 dihydrochloride

solid, ≥98% (HPLC)

Synonyme(s) :

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

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A propos de cet article

Formule empirique (notation de Hill) :
C14H17N3O2S · 2HCl
Numéro CAS:
Poids moléculaire :
364.29
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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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

SMILES string

Cl[H].Cl[H].O=S(=O)(N1CCCNCC1)c2cccc3cnccc23

InChI key

NOXXIYDYFSNHDF-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white to off-white

solubility

H2O: >10 mg/mL

Quality Level

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.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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Consulter la Bibliothèque de documents

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)
Leptin augments coronary vasoconstriction and smooth muscle proliferation via a Rho-kinase-dependent pathway
Noblet J N, et al.
Basic Research in Cardiology, 111(3), 25-25 (2016)
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
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
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

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