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
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 Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
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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)
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
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)
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)
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