ChemicalBook > CAS DataBase List > FASUDIL

FASUDIL

Product Name
FASUDIL
CAS No.
103745-39-7
Chemical Name
FASUDIL
Synonyms
at877;FASUDIL;Fasudilum;Fasudil HCI;HA-1077：Eril;FASUDIL USP/EP/BP;Fasudil Hydrchloride;Fasudil hydrochlorid;Fasudilum [inn-latin];H-1077 dihydrochloride
CBNumber
CB3101698
Molecular Formula
C14H17N3O2S
Formula Weight
291.37
MOL File
103745-39-7.mol
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FASUDIL Property

Boiling point:
506.2±60.0 °C(Predicted)
Density 
1.289±0.06 g/cm3(Predicted)
storage temp. 
Store at RT
solubility 
H2O: >200 mg/mL
form 
solid
pka
9.73±0.20(Predicted)
color 
white
Water Solubility 
Soluble in water or DMSO
CAS DataBase Reference
103745-39-7(CAS DataBase Reference)
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Safety

WGK Germany 
3
RTECS 
HM4031166
HS Code 
29334900
Toxicity
mouse,LD50,unreported,73500ug/kg (73.5mg/kg),United States Patent Document. Vol. #4678783,
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
371970
Product name
HA 1077, Dihydrochloride - CAS 103745-39-7 - Calbiochem
Packaging
1mg
Price
$159
Updated
2024/03/01
Alfa Aesar
Product number
J63525
Product name
Fasudil, 98+%
Packaging
10mg
Price
$243.65
Updated
2024/03/01
TRC
Product number
F150023
Product name
Fasudil
Packaging
100mg
Price
$165
Updated
2021/12/16
ApexBio Technology
Product number
B3523
Product name
Fasudil
Packaging
500mg
Price
$120
Updated
2021/12/16
ApexBio Technology
Product number
B3523
Product name
Fasudil
Packaging
200mg
Price
$70
Updated
2021/12/16
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FASUDIL Chemical Properties,Usage,Production

Chemical Properties

White Crystalline Solid

Uses

vasodilator (cerebral), Ca antagonist

Uses

A potent calcium antagonist vasodilator which is considered to act by employing different mechanisms from the usual calcium channel blockers since it inhibits (1) calcium ionophore A23187 induced co ntraction in arterial strips and (2) phenylephrine induced contraction in calcium free media suggesting that its site of action is in the intracellular space. Also reported to potently inhibit Rho- associated Kinase (ROCK IC50= 10.7 uM).

Uses

Fasudil is a protein kinase A inhibitor and may be used in medicinal combinations for hepatitis treatment.

Definition

ChEBI: Fasudil is an isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia. It has a role as a geroprotector, an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor, a vasodilator agent, a nootropic agent, a neuroprotective agent, an antihypertensive agent and a calcium channel blocker. It is a N-sulfonyldiazepane and a member of isoquinolines. It is a conjugate base of a fasudil(1+).

General Description

A cell-permeable, reversible, and ATP-competitive Ca2+ antagonist with anti-vasospastic properties. Inhibits protein kinase A (Ki = 1.6 μM), protein kinase G (Ki = 1.6 μM), and myosin light chain kinase (Ki = 3.6 μM). Also reported to potently inhibit Rho-associated kinase (ROCK; IC50 = 10.7 μM). Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency.

Biological Activity

Cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM). Ca2+ antagonist and vasodilator. Also inhibits proliferation of vascular smooth muscle cells.

Biochem/physiol Actions

Cell permeable: yes

in vitro

the inhibitory effects of fasudil on contractile responses to various agonists were examined on strips of rabbit aorta. the concentration-response curves to 5-hydroxytryptamine, prostaglandin f2alpha, histamine, angiotensin ii, noradrenaline and dopamine were concentration-dependently shifted to the right in the presence of fasudil [1].

in vivo

intra-coronary administration of fasudil to dog dose-dependently increased coronary blood flow, with no effect on mean blood pressure or heart rate. intra-coronary infusion of atropine, diphenhydramine or propranolol did not modify the in vivo coronary vasodilator response to fasudil [1].

References

[1] asano t, suzuki t, tsuchiya m, satoh s, ikegaki i, shibuya m, suzuki y, hidaka h. vasodilator actions of ha1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. br j pharmacol. 1989 dec;98(4):1091-100.
[2] zhao j, zhou d, guo j, ren z, zhou l, wang s, zhang y, xu b, zhao k, wang r, mao y, xu b, zhang x; fasudil aneurysmal subarachnoid hemorrhage study group. efficacy and safety of fasudil in patients with subarachnoid hemorrhage: final results of a randomized trial of fasudil versus nimodipine. neurol med chir (tokyo). 2011;51(10):679-83.

FASUDIL Preparation Products And Raw materials

Raw materials

Isoquinoline

Preparation Products

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FASUDIL Suppliers

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View Lastest Price from FASUDIL manufacturers

Hebei Guanlang Biotechnology Co,.LTD
Product
Fasudil 103745-39-7
Price
US $11.00/Kg/Bag
Min. Order
1g
Purity
99%
Supply Ability
10000kg
Release date
2021-07-02
Qiuxian Baitai New Material Co., LTD
Product
FASUDIL 103745-39-7
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
200000pcs
Release date
2021-03-17
Shaanxi Dideu Medichem Co. Ltd
Product
Fasudil 103745-39-7
Price
US $0.00-0.00/KG
Min. Order
1KG
Purity
99.0%
Supply Ability
500 MT
Release date
2020-05-11

103745-39-7, FASUDILRelated Search:

5-Quinolinesulfonic acid, 2-methyl- CINITAPRIDE HYDROGEN TARTRATE Fosaprepitant dimeglumine CAL-101 Temsirolimus Rapamycin Ripasudil Icotinib Radotinib Oxiracetam Nimodipine FASUDIL 1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride Fasudil Monohydrochloride,FASUDIL HCL,FASUDIL HYDROCHLORIDE,FASUDIL DIHYDROCHLORIDE H-1152Glycyl, Dihydrochloride 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE HA1077 (Fasudil)

  • Fasudil Hydrochloride Injection
  • 5-(AZEPAN-4-YLSULFONYL)ISOQUINOLINE DIHYDROCHLORIDE
  • Fasudil HCI
  • 5-(1,4-diazepan-4-ium-1-ylsulfonyl)isoquinoline
  • Fasudil Hydrchloride
  • 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE
  • at877
  • hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine
  • HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE
  • HA 1077, DIHYDROCHLORIDE, 99+%
  • FASUDIL
  • Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine
  • 1H-1,4-Diazepine, hexahydro-1-(5-isoquinolinylsulfonyl)-
  • Fasudilum
  • Fasudilum [inn-latin]
  • HA-1077：Eril
  • 2,3,4,5,6,7-Hexahydro-1-(isoquinolin-5-ylsulfonyl)-1H-1,4-diazepine
  • 5-(Hexahydro-1H-1,4-diazepine-1-ylsulfonyl)isoquinoline
  • H-1077 dihydrochloride
  • HA-1077 Dihydrochloride Salt >99%
  • 1-(5-Isoquinolinesulfonyl)homopiperazine, Dihydrochloride Salt
  • 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline dihydrochloride
  • Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-
  • FASUDIL USP/EP/BP
  • Fasudil hydrochlorid
  • High Quality API Intermediate Fasudil
  • (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE
  • 103745-39-7
  • C14H17N3O2S2HCl
  • C14H17N3O2S2ClH
  • Signalling
  • Protein Kinase Inhibitors and Activators
  • Protein Kinase
  • Angiogenesis and Metastasis
  • Intracellular signaling
  • ERIL
  • APIs