Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C14H17N3O2S.CH4O3S |
| Molecular Weight | 387.474 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.O=S(=O)(N1CCCNCC1)C2=CC=CC3=C2C=CN=C3
InChI
InChIKey=MVCDPGYHRHUECK-UHFFFAOYSA-N
InChI=1S/C14H17N3O2S.CH4O3S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;1-5(2,3)4/h1,3-5,7,11,15H,2,6,8-10H2;1H3,(H,2,3,4)
| Molecular Formula | CH4O3S |
| Molecular Weight | 96.106 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C14H17N3O2S |
| Molecular Weight | 291.369 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2111459 |
0.4 µM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | ERIL Approved UseImprovement of cerebral vasospasm and cerebral ischemic symptoms associated with cerebral vasospasm after subarachnoid hemorrhage. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Hypoxia and Rho/Rho-kinase signaling. Lung development versus hypoxic pulmonary hypertension. | 2003 |
|
| 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 |
|
| 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 |
|
| Effects of the Rho-kinase inhibitors, Y-27632 and fasudil, on the corpus cavernosum from diabetic mice. | 2003 Jul 11 |
|
| 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 |
|
| Expression of Rho-kinase and its functional role in the contractile activity of the mouse vas deferens. | 2003 Oct |
|
| Long-term inhibition of Rho-kinase suppresses angiotensin II-induced cardiovascular hypertrophy in rats in vivo: effect on endothelial NAD(P)H oxidase system. | 2003 Oct 17 |
|
| Effects of HA-1077 and Y-27632, two rho-kinase inhibitors, in the human umbilical artery. | 2004 |
|
| Regulation of osteoblast differentiation by Pasteurella multocida toxin (PMT): a role for Rho GTPase in bone formation. | 2004 Apr |
|
| [Development of drug delivery system for intrathecal administration and its therapeutic effect on cerebral vasospasm and ischemia]. | 2004 Aug |
|
| Involvement of Rho-kinase in cold ischemia-reperfusion injury after liver transplantation in rats. | 2004 Aug 15 |
|
| 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 |
|
| Long-term inhibition of Rho-kinase suppresses left ventricular remodeling after myocardial infarction in mice. | 2004 May 11 |
|
| Rho kinase mediates cold-induced constriction of cutaneous arteries: role of alpha2C-adrenoceptor translocation. | 2004 May 28 |
|
| Role of the Rhoa/Rho kinase system in flow-related remodeling of rat mesenteric small arteries in vivo. | 2004 May-Jun |
|
| 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 |
|
| [Inhibition of Rho-kinase by fasudil preventing anginal attacks associated with spastic angina: a case report]. | 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 |
|
| Inhibition of Rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection. | 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. | 2005 |
|
| 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 |
|
| Rho-kinase and myosin II activities are required for cell type and environment specific migration. | 2005 Feb |
|
| Prostacyclin does not inhibit rho-kinase: an implication for the treatment of pulmonary hypertension. | 2005 Feb |
|
| [Role of calcium desensitization in vascular hyporeactivity in hemorrhagic shock]. | 2005 Jan |
|
| 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 |
|
| Fasudil prevents KATP channel-induced improvement in postischemic functional recovery. | 2005 Jun |
|
| 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 |
|
| Acute vasodilator effects of a Rho-kinase inhibitor, fasudil, in patients with severe pulmonary hypertension. | 2005 Mar |
|
| Inhaled Rho kinase inhibitors are potent and selective vasodilators in rat pulmonary hypertension. | 2005 Mar 1 |
|
| 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 |
Patents
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
Created
by
admin
on
Edited
Sat Dec 16 18:16:10 GMT 2023
by
admin
on
Sat Dec 16 18:16:10 GMT 2023
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| Record UNII |
4S5NTB667B
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| Record Status |
Validated (UNII)
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| Record Version |
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300000017638
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1001206-62-7
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4S5NTB667B
Created by
admin on Sat Dec 16 18:16:10 GMT 2023 , Edited by admin on Sat Dec 16 18:16:10 GMT 2023
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