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105628-72-6 | 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE
CAS No: 105628-72-6 Catalog No: AG008RE1 MDL No:MFCD01752417
Product Description
Catalog Number:
AG008RE1
Chemical Name:
1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE
CAS Number:
105628-72-6
Molecular Formula:
C14H17N3O3S
Molecular Weight:
307.3681
MDL Number:
MFCD01752417
IUPAC Name:
5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one
InChI:
InChI=1S/C14H17N3O3S/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17/h1,3-5,7,15H,2,6,8-10H2,(H,16,18)
InChI Key:
ZAVGJDAFCZAWSZ-UHFFFAOYSA-N
SMILES:
O=c1[nH]ccc2c1cccc2S(=O)(=O)N1CCNCCC1
Properties
Complexity:
526
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
307.099g/mol
Formal Charge:
0
Heavy Atom Count:
21
Hydrogen Bond Acceptor Count:
5
Hydrogen Bond Donor Count:
2
Isotope Atom Count:
0
Molecular Weight:
307.368g/mol
Monoisotopic Mass:
307.099g/mol
Rotatable Bond Count:
2
Topological Polar Surface Area:
86.9A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
0.2
Literature
| Title | Journal |
|---|---|
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| Hydroxyfasudil ameliorates bladder dysfunction in male spontaneously hypertensive rats. | Urology 20120501 |
| Long-term treatment with nifedipine suppresses coronary hyperconstricting responses and inflammatory changes induced by paclitaxel-eluting stent in pigs in vivo: possible involvement of Rho-kinase pathway. | European heart journal 20120301 |
| Propofol neurotoxicity is mediated by p75 neurotrophin receptor activation. | Anesthesiology 20120201 |
| Inhibition of Rho kinase by hydroxyfasudil attenuates brain edema after subarachnoid hemorrhage in rats. | Neurochemistry international 20120201 |
| Antivasospastic effects of hydroxyfasudil, a Rho-kinase inhibitor, after subarachnoid hemorrhage. | Journal of pharmacological sciences 20120101 |
| High-dose fasudil preserves postconditioning against myocardial infarction under hyperglycemia in rats: role of mitochondrial KATP channels. | Cardiovascular diabetology 20120101 |
| Protein phosphatase 1 dephosphorylates profilin-1 at Ser-137. | PloS one 20120101 |
| Pirfenidone inhibits transforming growth factor-β1-induced fibrogenesis by blocking nuclear translocation of Smads in human retinal pigment epithelial cell line ARPE-19. | Molecular vision 20120101 |
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| Ca2+ sensitization and PKC contribute to exercise training-enhanced contractility in porcine collateral-dependent coronary arteries. | American journal of physiology. Heart and circulatory physiology 20110401 |
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| Dynamic changes in neurexins' alternative splicing: role of Rho-associated protein kinases and relevance to memory formation. | PloS one 20110101 |
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| Hydroxyfasudil-mediated inhibition of ROCK1 and ROCK2 improves kidney function in rat renal acute ischemia-reperfusion injury. | PloS one 20110101 |
| ROCKing Regeneration: Rho Kinase Inhibition as Molecular Target for Neurorestoration. | Frontiers in molecular neuroscience 20110101 |
| Mutant huntingtin alters cell fate in response to microtubule depolymerization via the GEF-H1-RhoA-ERK pathway. | The Journal of biological chemistry 20101126 |
| Simultaneous quantitative analysis of fasudil and its active metabolite in human plasma by liquid chromatography electro-spray tandem mass spectrometry. | Journal of pharmaceutical and biomedical analysis 20100605 |
| Effects of sex and estrogen on chicken ductus arteriosus reactivity. | American journal of physiology. Regulatory, integrative and comparative physiology 20100501 |
| Role of Rho-kinase in mediating contraction of chicken embryo femoral arteries. | Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology 20100301 |
| Abstracts of the 16th Annual Society on NeuroImmune Pharmacology (SNIP) Conference. April 13-17, 2010. Manhattan Beach, California, USA. | Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology 20100301 |
| Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase. | Journal of medicinal chemistry 20100128 |
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| Recent development of cyclic amide (pyridone/lactam) moiety containing heterocycles as protein kinase inhibitors. | Current medicinal chemistry 20100101 |
| Characterization of dysferlin deficient SJL/J mice to assess preclinical drug efficacy: fasudil exacerbates muscle disease phenotype. | PloS one 20100101 |
| The role of RhoA/Rho kinase pathway in endothelial dysfunction. | Journal of cardiovascular disease research 20100101 |
| Role of Rho-kinase in the pathogenesis of coronary hyperconstricting responses induced by drug-eluting stents in pigs in vivo. | Journal of the American College of Cardiology 20091208 |
| Maturation of O2 sensing and signaling in the chicken ductus arteriosus. | American journal of physiology. Lung cellular and molecular physiology 20091001 |
| Effect of the rho-kinase inhibitor hydroxyfasudil on bladder overactivity: an experimental rat model. | International journal of urology : official journal of the Japanese Urological Association 20091001 |
| Evidence for Rho-kinase activation in patients with pulmonary arterial hypertension. | Circulation journal : official journal of the Japanese Circulation Society 20090901 |
| Simvastatin suppresses leptin expression in 3T3-L1 adipocytes via activation of the cyclic AMP-PKA pathway induced by inhibition of protein prenylation. | Journal of biochemistry 20090601 |
| Remote periconditioning reduces myocardial no-reflow by the activation of K ATP channel via inhibition of Rho-kinase. | International journal of cardiology 20090403 |
| A role for Rho-kinase in Ca-independent contractions induced by phorbol-12,13-dibutyrate. | Clinical and experimental pharmacology & physiology 20090301 |
| Morphological and functional alterations of the ductus arteriosus in a chicken model of hypoxia-induced fetal growth retardation. | Pediatric research 20090301 |
| Peripheral delivery of a ROCK inhibitor improves learning and working memory. | Behavioral neuroscience 20090201 |
| RhoA/Rho-kinase signaling: a therapeutic target in pulmonary hypertension. | Vascular health and risk management 20090101 |
| Dopamine D2 receptor stimulation potentiates PolyQ-Huntingtin-induced mouse striatal neuron dysfunctions via Rho/ROCK-II activation. | PloS one 20090101 |
| Substrate stiffness affects the functional maturation of neonatal rat ventricular myocytes. | Biophysical journal 20081001 |
| Potent inhibition of cicatricial contraction in proliferative vitreoretinal diseases by statins. | Diabetes 20081001 |
| Rho kinase-dependent CCL20 induced by dynamic compression of human chondrocytes. | Arthritis and rheumatism 20080901 |
| Improvement of cognitive deficit and neuronal damage in rats with chronic cerebral ischemia via relative long-term inhibition of rho-kinase. | Cellular and molecular neurobiology 20080801 |
| Safety and efficacy of fasudil monotherapy and fasudil-ozagrel combination therapy in patients with subarachnoid hemorrhage: sub-analysis of the post-marketing surveillance study. | Neurologia medico-chirurgica 20080601 |
| The therapeutic effects of Rho-ROCK inhibitors on CNS disorders. | Therapeutics and clinical risk management 20080601 |
| Wide therapeutic time window for Rho-kinase inhibition therapy in ischemic brain damage in a rat cerebral thrombosis model. | Brain research 20080208 |
| Contraction of tubulointerstitial fibrosis tissue in diabetic nephropathy, as demonstrated in an in vitro fibrosis model. | Virchows Archiv : an international journal of pathology 20071101 |
| The role of HMG-CoA reductase inhibition in endothelial dysfunction and inflammation. | Vascular health and risk management 20071001 |
| Fasudil, a Rho kinase (ROCK) inhibitor, protects against ischemic neuronal damage in vitro and in vivo by acting directly on neurons. | Brain research 20070618 |
| [Regulatory effects of RhoGTPase on transition of liver sinusoidal capillarization: experiment with mice of schistosomal hepatic fibrosis]. | Zhonghua yi xue za zhi 20070612 |
| Rho-kinase inhibition acutely augments blood flow in focal cerebral ischemia via endothelial mechanisms. | Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20070501 |
| Acute vasodilator effect of fasudil, a Rho-kinase inhibitor, in monocrotaline-induced pulmonary hypertension in rats. | Journal of cardiovascular pharmacology 20070201 |
| Wide therapeutic time window for fasudil neuroprotection against ischemia-induced delayed neuronal death in gerbils. | Brain research 20070112 |
| Different migration of vascular smooth muscle cells from human coronary artery bypass vessels. Role of Rho/ROCK pathway. | Journal of vascular research 20070101 |
| Sustained elevation of serum cortisol level causes sensitization of coronary vasoconstricting responses in pigs in vivo: a possible link between stress and coronary vasospasm. | Circulation research 20060929 |
| 8-Isoprostane-induced endothelin-1 production by infant rat pulmonary artery smooth muscle cells is mediated by Rho-kinase. | Free radical biology & medicine 20060915 |
| Long-term inhibition of Rho kinase suppresses intimal thickening in autologous vein grafts in rabbits. | Journal of vascular surgery 20060601 |
| Determination of the enantiomeric excess of an M3 antagonist drug substance by chemometric analysis of the IR spectra of different guest-host complexes. | Chirality 20060515 |
| Critical role of the Rho-kinase pathway in TGF-beta2-dependent collagen gel contraction by retinal pigment epithelial cells. | Experimental eye research 20060501 |
| The structure of dimeric ROCK I reveals the mechanism for ligand selectivity. | The Journal of biological chemistry 20060106 |
| Rho-kinase as a molecular target for insulin resistance and hypertension. | FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20060101 |
| Cardioprotective effect of hydroxyfasudil as a specific Rho-kinase inhibitor, on ischemia-reperfusion injury in canine coronary microvessels in vivo. | Clinical hemorheology and microcirculation 20060101 |
| Statins prevent pulsatile stretch-induced proliferation of human saphenous vein smooth muscle cells via inhibition of Rho/Rho-kinase pathway. | Cardiovascular research 20051201 |
| Effects of fasudil in acute ischemic stroke: results of a prospective placebo-controlled double-blind trial. | Journal of the neurological sciences 20051115 |
| Inhibition of rho-kinase by hydroxyfasudil prevents vasopressin-induced myocardial ischemia in Donryu rats by attenuating coronary vasoconstriction. | Pharmacology 20051101 |
| Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection. | Stroke 20051001 |
| Rho-kinase mediates hyperglycemia-induced plasminogen activator inhibitor-1 expression in vascular endothelial cells. | Circulation 20050621 |
| Age-related differences in vasoconstrictor responses to isoprostanes in piglet pulmonary and mesenteric vascular smooth muscle. | Pediatric research 20050601 |
| Beneficial effect of hydroxyfasudil, a specific Rho-kinase inhibitor, on ischemia/reperfusion injury in canine coronary microcirculation in vivo. | Journal of the American College of Cardiology 20050215 |
| Prostacyclin does not inhibit rho-kinase: an implication for the treatment of pulmonary hypertension. | Journal of cardiovascular pharmacology 20050201 |
| Effects of hydroxyfasudil administered to the nucleus tractus solitarii on blood pressure and heart rate in spontaneously hypertensive rats. | Clinical and experimental hypertension (New York, N.Y. : 1993) 20050101 |
| Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss. | BMC ear, nose, and throat disorders 20050101 |
| Chronologic changes of fasudil hydrochloride and hydroxyfasudil in cerebrospinal fluid of patients with aneurysmal subarachnoid hemorrhage. | Journal of stroke and cerebrovascular diseases : the official journal of National Stroke Association 20050101 |
| The involvement of the rho-kinase pathway and its regulation in cytokine-induced collagen gel contraction by hyalocytes. | Investigative ophthalmology & visual science 20041101 |
| Inhibition of Rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection. | Arteriosclerosis, thrombosis, and vascular biology 20041001 |
| Protein kinase A as another mediator of ischemic preconditioning independent of protein kinase C. | Circulation 20040706 |
| Long-term inhibition of Rho-kinase suppresses left ventricular remodeling after myocardial infarction in mice. | Circulation 20040511 |
| Remnant lipoproteins from patients with sudden cardiac death enhance coronary vasospastic activity through upregulation of Rho-kinase. | Arteriosclerosis, thrombosis, and vascular biology 20040501 |
| Long-term treatment with a Rho-kinase inhibitor improves monocrotaline-induced fatal pulmonary hypertension in rats. | Circulation research 20040220 |
| [Rho-kinase inhibitor]. | Nihon rinsho. Japanese journal of clinical medicine 20040201 |
| Long-term treatment with a specific Rho-kinase inhibitor suppresses cardiac allograft vasculopathy in mice. | Circulation research 20040109 |
| Evidence for protein kinase C-mediated activation of Rho-kinase in a porcine model of coronary artery spasm. | Arteriosclerosis, thrombosis, and vascular biology 20031201 |
| Long-term inhibition of Rho-kinase suppresses angiotensin II-induced cardiovascular hypertrophy in rats in vivo: effect on endothelial NAD(P)H oxidase system. | Circulation research 20031017 |
| Essential role of rho kinase in the Ca2+ sensitization of prostaglandin F(2alpha)-induced contraction of rabbit aortae. | The Journal of physiology 20030201 |
| Fasudil attenuates interstitial fibrosis in rat kidneys with unilateral ureteral obstruction. | European journal of pharmacology 20021129 |
| Anti-anginal effect of fasudil, a Rho-kinase inhibitor, in patients with stable effort angina: a multicenter study. | Journal of cardiovascular pharmacology 20021101 |
| [Involvement of Rho-kinase in hypertensive vascular disease--a novel therapeutic target in hypertension]. | Fukuoka igaku zasshi = Hukuoka acta medica 20020801 |
| Rho-kinase mediates hypoxia-induced downregulation of endothelial nitric oxide synthase. | Circulation 20020702 |
| Rho-kinase as a novel therapeutic target in treatment of cardiovascular diseases. | Journal of cardiovascular pharmacology 20020301 |
| Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries. | Arteriosclerosis, thrombosis, and vascular biology 20020201 |
| Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. | British journal of pharmacology 20011201 |
| Pitavastatin enhanced BMP-2 and osteocalcin expression by inhibition of Rho-associated kinase in human osteoblasts. | Biochemical and biophysical research communications 20010921 |
| Involvement of Rho-kinase in vascular remodeling caused by long-term inhibition of nitric oxide synthesis in rats. | European journal of pharmacology 20010907 |
| Long-term inhibition of Rho-kinase induces a regression of arteriosclerotic coronary lesions in a porcine model in vivo. | Cardiovascular research 20010701 |
| Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase. | Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism 20010701 |
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