FASUDIL

FASUDIL Basic information
Product Name:FASUDIL
Synonyms:Fasudil Hydrochloride Injection;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
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
FASUDIL Structure
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
pka9.73±0.20(Predicted)
color white
Water Solubility Soluble in water or DMSO
CAS DataBase Reference103745-39-7(CAS DataBase Reference)
Safety Information
WGK Germany 3
RTECS HM4031166
HS Code 29334900
Toxicitymouse,LD50,unreported,73500ug/kg (73.5mg/kg),United States Patent Document. Vol. #4678783,
MSDS Information
FASUDIL Usage And Synthesis
Chemical PropertiesWhite Crystalline Solid
UsesA 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).
Usesvasodilator (cerebral), Ca antagonist
UsesFasudil is a protein kinase A inhibitor and may be used in medicinal combinations for hepatitis treatment.
DefinitionChEBI: 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 DescriptionA 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 ActivityCyclic 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 ActionsCell permeable: yes
in vitrothe 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 vivointra-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 materialsIsoquinoline
Preparation ProductsFasudil hydrochloride
Rapamycin Nimodipine Radotinib Oxiracetam 5-Quinolinesulfonic acid, 2-methyl- Temsirolimus Fosaprepitant dimeglumine CAL-101 Icotinib CINITAPRIDE HYDROGEN TARTRATE Ripasudil H-1152Glycyl, Dihydrochloride 1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride (S)-(+)-2-METHYL-1-[(4-METHYL-5-ISOQUINOLYNYL)SULFONYL]HOMOPIPERAZINE FASUDIL Fasudil Monohydrochloride,FASUDIL HCL,FASUDIL HYDROCHLORIDE,FASUDIL DIHYDROCHLORIDE 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE HA1077 (Fasudil)

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