FASUDIL

ChemicalBook > CAS DataBase List > 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 (K_i = 1.6 μM), protein kinase G (K_i = 1.6 μM), and myosin light chain kinase (K_i = 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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View Lastest Price from FASUDIL manufacturers

Hebei Chuanghai Biotechnology Co,.LTD

Product: Fasudil 103745-39-7
Price: US $11.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 10000kg
Release date: 2024-08-21

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

HA-1077 (Fasudil) (mM/ml), ROCK2 inhibitor

103745-39-7

C14H17N3O2S2HCl

C14H17N3O2S2ClH

Signalling

Protein Kinase Inhibitors and Activators

Protein Kinase

Angiogenesis and Metastasis

Intracellular signaling

ERIL

APIs