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H139

Sigma-Aldrich

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:
203911-27-7
Molecular Weight:
364.29
MDL number:
MFCD00153805
UNSPSC Code:
12352200
PubChem Substance ID:
24895456
NACRES:
NA.77

Quality Level

100

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

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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)
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
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)
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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