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Stereochemistry ACHIRAL
Molecular Formula C14H17N3O2S.CH4O3S
Molecular Weight 387.474
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0







Molecular Formula C14H17N3O2S
Molecular Weight 291.369
Charge 0
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula CH4O3S
Molecular Weight 96.106
Charge 0
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Fasudil is a potent Rho kinase inhibitor, which was developed by Asahi Kasei. The drug is used in Asia for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage.

Approval Year



Primary TargetPharmacologyConditionPotency
0.4 µM [Ki]


ConditionModalityTargetsHighest PhaseProduct

Approved Use

Improvement of cerebral vasospasm and cerebral ischemic symptoms associated with cerebral vasospasm after subarachnoid hemorrhage.


Protein kinases--the major drug targets of the twenty-first century?
2002 Apr
[Basic and clinical studies on coronary vasospasm].
2002 Dec
The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway.
2002 Feb-Mar
Membrane depolarization-induced contraction of rat caudal arterial smooth muscle involves Rho-associated kinase.
2002 Jun 1
Inhibition of Rho/Rho-kinase signaling downregulates plasminogen activator inhibitor-1 synthesis in cultured human monocytes.
2002 Jun 12
Effects of Rho-kinase inhibitor on vasopressin-induced chronic myocardial damage in rats.
2002 Nov 22
The mechanism of excitation-contraction coupling in phenylephrine-stimulated human saphenous vein.
2002 Oct
Nitric oxide-induced motility in aortic smooth muscle cells: role of protein tyrosine phosphatase SHP-2 and GTP-binding protein Rho.
2002 Sep 6
Hypoxia and Rho/Rho-kinase signaling. Lung development versus hypoxic pulmonary hypertension.
Involvement of Rho/Rho-kinase signalling in the contractile activity and acetylcholine release in the mouse gastric fundus.
2003 Apr 11
Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm.
2003 Apr 18
Hyperosmotic-induced protein kinase N 1 activation in a vesicular compartment is dependent upon Rac1 and 3-phosphoinositide-dependent kinase 1.
2003 Aug 22
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity.
2003 Dec
Effect of fasudil on Rho-kinase and nephropathy in subtotally nephrectomized spontaneously hypertensive rats.
2003 Dec
Rho kinase inhibitors block activation of pancreatic stellate cells.
2003 Dec
Comparison of signalling mechanisms involved in rat mesenteric microvessel contraction by noradrenaline and sphingosylphosphorylcholine.
2003 Jan
Effects of the Rho-kinase inhibitors, Y-27632 and fasudil, on the corpus cavernosum from diabetic mice.
2003 Jul 11
P2X7 receptor-dependent blebbing and the activation of Rho-effector kinases, caspases, and IL-1 beta release.
2003 Jun 1
Protein kinase C is necessary for recovery from the thyrotropin-releasing hormone-induced r-ERG current reduction in GH3 rat anterior pituitary cells.
2003 Mar 15
Smoking activates rho-kinase in smooth muscle cells of forearm vasculature in humans.
2003 May
Vessel- and vasoconstrictor-dependent role of rho/rho-kinase in renal microvascular tone.
2003 May-Jun
Effects of HA-1077 and Y-27632, two rho-kinase inhibitors, in the human umbilical artery.
Regulation of osteoblast differentiation by Pasteurella multocida toxin (PMT): a role for Rho GTPase in bone formation.
2004 Apr
Involvement of RhoA and possible neuroprotective effect of fasudil, a Rho kinase inhibitor, in NMDA-induced neurotoxicity in the rat retina.
2004 Aug 20
[Rho-kinase inhibitor].
2004 Feb
Long-term treatment with a Rho-kinase inhibitor improves monocrotaline-induced fatal pulmonary hypertension in rats.
2004 Feb 20
Rho-kinase expression and its contribution to the control of perfusion pressure in the isolated rat mesenteric vascular bed.
2004 Feb 6
Differential effects of Rho-kinase inhibition on artery wall mass and remodeling.
2004 Jan
Long-term inhibition of Rho-kinase suppresses neointimal formation after stent implantation in porcine coronary arteries: involvement of multiple mechanisms.
2004 Jan
Long-term treatment with a specific Rho-kinase inhibitor suppresses cardiac allograft vasculopathy in mice.
2004 Jan 9
The Rho-ROCK system as a new therapeutic target for preventing interstitial fibrosis.
2004 Jan-Feb
[Involvement of small GTPase Rho and Rho-kinase in the pathogenesis of hypertension and hypertensive target organ damage].
2004 Mar
Involvement of RhoA and Rho kinase in neutrophil-stimulated endothelial hyperpermeability.
2004 Mar
Inhibition of protein kinase C-mediated contraction by Rho kinase inhibitor fasudil in rabbit aorta.
2004 Nov
Rho-kinase, a potential therapeutic target for the treatment of hypertension.
2004 Oct
Expression of Rho-kinase (ROCK-1 and ROCK-2) and its substantial role in the contractile activity of the sheep ureter.
2004 Oct
Usefulness of fasudil, a Rho-kinase inhibitor, to treat intractable severe coronary spasm after coronary artery bypass surgery.
2004 Sep
Fasudil, a Rho-kinase inhibitor, attenuates glomerulosclerosis in Dahl salt-sensitive rats.
2004 Sep
Mechanisms underlying postjunctional synergism between responses of the vas deferens to noradrenaline and ATP.
2004 Sep 13
Therapeutic potential of rho-kinase inhibitors in cardiovascular diseases.
Role of Rho-kinase and p27 in angiotensin II-induced vascular injury.
2005 Apr
Long term Rho-kinase inhibition ameliorates endothelial dysfunction in LDL-Receptor deficient mice.
2005 Apr 11
Inhibition of Rho-kinase by fasudil attenuated angiotensin II-induced cardiac hypertrophy in apolipoprotein E deficient mice.
2005 Apr 11
Stent implantation activates RhoA in human arteries: inhibitory effect of rapamycin.
2005 Jan-Feb
Statins decrease Toll-like receptor 4 expression and downstream signaling in human CD14+ monocytes.
2005 Jul
Activation of Rho-associated kinase during augmented contraction of the basilar artery to serotonin after subarachnoid hemorrhage.
2005 Jun
High-throughput screening for kinase inhibitors.
2005 Mar
Small guanine nucleotide-binding protein Rho and myocardial function.
2005 Mar
Negative regulation of RhoA/Rho kinase by angiotensin II type 2 receptor in vascular smooth muscle cells: role in angiotensin II-induced vasodilation in stroke-prone spontaneously hypertensive rats.
2005 May
Fasudil, a Rho-kinase inhibitor, attenuates angiotensin II-induced abdominal aortic aneurysm in apolipoprotein E-deficient mice by inhibiting apoptosis and proteolysis.
2005 May 3

Sample Use Guides

The recommended dosage is 30 mg fasudil hydrochloride should be diluted in 50-100 mL solution and administered by intravenous infusion over 30 minutes 2-3 times daily.
Route of Administration: Intravenous
The rat aortic rings were contracted by KCl; when the contraction reached a plateau, fasudil was added at concentrations from 10(-9) to 10(-5) M. The relaxation IC50 was 0.74 uM. When rabbit aortic rings were used, IC50 values were 37,15 uM and 27,54 uM for KCl and Methoxamine-induced contraction, respectively.
Substance Class Chemical
by admin
on Thu Jul 06 23:33:27 UTC 2023
by admin
on Thu Jul 06 23:33:27 UTC 2023
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Common Name English
Common Name English
Fasudil mesilate [WHO-DD]
Common Name English
Systematic Name English
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Created by admin on Thu Jul 06 23:33:27 UTC 2023 , Edited by admin on Thu Jul 06 23:33:27 UTC 2023
Created by admin on Thu Jul 06 23:33:27 UTC 2023 , Edited by admin on Thu Jul 06 23:33:27 UTC 2023
Created by admin on Thu Jul 06 23:33:27 UTC 2023 , Edited by admin on Thu Jul 06 23:33:27 UTC 2023
Created by admin on Thu Jul 06 23:33:27 UTC 2023 , Edited by admin on Thu Jul 06 23:33:27 UTC 2023
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