Fasudil

Modify Date: 2024-01-02 17:38:48

Fasudil structure	Common Name	Fasudil
	CAS Number	103745-39-7	Molecular Weight	291.37
	Density	1.3±0.1 g/cm3	Boiling Point	506.2±60.0 °C at 760 mmHg
	Molecular Formula	C₁₄H₁₇N₃O₂S	Melting Point	N/A
	MSDS	N/A	Flash Point	259.9±32.9 °C

Use of Fasudil

Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Name	fasudil
Synonym	More Synonyms

Description	Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA Signaling Pathways >> Stem Cell/Wnt >> PKA Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK Research Areas >> Cancer
Target	p160ROCK:0.33 μM (Ki) PKA:1 μM (Ki) PKC:9.3 μM (Ki) MLCK:55 μM (Ki)
In Vitro	Fasudil has vasodilatory action and occupies the adenine pocket of the ATP-binding site of the enzyme[1]. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil inhibits contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a[2]. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction[3]. In addition, Fasudil induces disorganization of actin stress fiber and cell migration inhibition[4]. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil also blocks the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK[5].
In Vivo	Fasudil (30 μg) increases CBF by 50% via intra-coronary injection to dogs. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs[3]. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6]. Fasudil (100 mg/kg/day, p.o.) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration[7].
Kinase Assay	Cyclic AMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HCl (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cyclic AMP or absence of cyclic AMP, 3.3 to 20 μM [r-32P] ATP (4×105 c.p.m.), 0.5 μg of the enzyme, 100 μg of histone H2B and compound. The mixture is incubated at 30°C for 5 min. The reaction is terminated by adding 1mL of ice-cold 20% trichloroacetic acid after adding 500 μg of bovine serum albumin as a carrier protein. The sample is centrifuged at 3000 r.p.m. for 15min, the pellet is resuspended in ice-cold 10% trichloro-acetic acid solution and the centrifugation-resuspension cycle is repeated three times. The final pellet is dissolved in 1 mL of 1 N NaOH and radioactivity is measured with a liquid scintillation counter[1].
References	[1]. Ono-Saito N, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31. [2]. Asano T, et al. Mechanism of action of a novel antivasospasm drug, HA1077. J Pharmacol Exp Ther. 1987 Jun;241(3):1033-40. [3]. Asano T, et al. 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. [4]. Negoro N, et al. The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Aug 19;262(1):211-5. [5]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38. [6]. Zhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80. [7]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. [8]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4.

Density	1.3±0.1 g/cm3
Boiling Point	506.2±60.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₇N₃O₂S
Molecular Weight	291.37
Flash Point	259.9±32.9 °C
PSA	70.68000
LogP	1.19
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.622
Storage condition	Store at RT
Water Solubility	H2O: >200 mg/mL

WGK Germany	3
RTECS	HM4031166
HS Code	2933990090

Homopiperazine

CAS#:505-66-8

ISOQUINOLINE-5-...

CAS#:84468-15-5

~88%

Fasudil

CAS#:103745-39-7

Literature: Asahi Kasei Kogyo Kabushiki Kaisha Patent: US5942505 A1, 1999 ;

Homopiperazine

CAS#:505-66-8

Isoquinoline-5-...

CAS#:105627-79-0

~89%

Fasudil

CAS#:103745-39-7

Literature: Asahi Kasei Kogyo Kabushiki Kaisha Patent: US4678783 A1, 1987 ; US 4678783 A

Precursor 3
CAS#:505-66-8 Homopiperazine CAS#:84468-15-5 ISOQUINOLINE-5-... CAS#:105627-79-0 Isoquinoline-5-...
DownStream 1
CAS#:105628-07-7 Fasudil Hydroch...

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Fasudilum [inn-latin]

H-1077 dihydrochloride

1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine,Dihydrochloride

1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE

HA 1077,DIHYDROCHLORIDE

5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline

HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE

Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-

at877

5-(1,4-DIAZEPAN-1-SULFONYL)ISOQUINOLINE

Fasudilum

1-(5-Isoquinolinylsulfonyl)homopiperazine

Fasudil

MFCD00866182

hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine

1-(5-isoquinolinesulphonyl)-homopiperazine

1-(5-Isoquinolinesulphonyl)homopiperazine

N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine

(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE

DC Chemicals Limited
China
Product Name: Fasudil
Price: $350.0/1g
Purity: 98.0%
Stocking Period: Inquiry
Contact: Tony Cao

Zhejiang Hangyu API Co., Ltd
China
Product Name: FASUDIL
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: FASUDIL
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

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Fasudil

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