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FASUDIL

Basic information Safety Supplier Related

FASUDIL Basic information

Product Name:
FASUDIL
Synonyms:
  • 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
CAS:
103745-39-7
MF:
C14H17N3O2S
MW:
291.37
EINECS:
816-154-4
Product Categories:
  • Signalling
  • Protein Kinase Inhibitors and Activators
  • Protein Kinase
  • Angiogenesis and Metastasis
  • Intracellular signaling
  • ERIL
  • APIs
Mol File:
103745-39-7.mol
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FASUDIL Chemical Properties

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 Information

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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FASUDIL Usage And Synthesis

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

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