Fasudil hydrochloride Basic information
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Product Name: |
Fasudil hydrochloride |
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Synonyms: |
1-(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE HYDROCHLORIDE;Fasudil Monohydrochloride;(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE, 2HCL;5-(1,4-DIAZEPAN-1-YLSULFONYL)ISOQUINOLINE HYDROCHLORIDE;HEXAHYDRO-1-(5-ISOQUINOLINYLSULFONYL)-MONOHYDROCHLORIDE;HA-1077;HA-1077 DIHYDROCHLORIDE;FASUDEL |
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CAS: |
105628-07-7 |
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MF: |
C14H18ClN3O2S |
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MW: |
327.83 |
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EINECS: |
805-833-0 |
Fasudil hydrochloride Physical and Chemical Properties
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Melting point |
220.5 °C;mp 219.3°(Shirotani) |
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Solubility |
H2O:>200mg/mL |
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Storage Condition |
Inert atmosphere,Store in freezer, under -20°C |
| Color | white |
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Form |
Solid |
| Water Solubility | Soluble in water and dimethyl sulfoxide. Insoluble in ethanol. |
| Merck | 14,3942 |
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Stability |
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month. |
Fasudil hydrochloride Usage
| Description | Fasudil hydrochloride, a novel calcium antagonistic vasodilator, was marketed for the treatment of cerebral vasospasm following subarachnoid hemorrhage (SAH). Fasudil is also a potent inhibitor of myosin light chain kinase and protein kinase C. In contrast to other calcium channel blockers, which regulate the influx of calcium ions through the cell membrane but not involved in the intracellular regulatory mechanism of the calcium, fasudil was suggested to have an intracellular mode of action in relaxing vascular smooth muscle. In patients with neurological deficits due to vasospasm, fasudil decreased the occurrence of angiographic severe and symptomatic vasospasm and cerebral infarction without decreasing systemic blood pressure. Fasudil is reportedly in clinical trials for acute ischemic stroke, sequelae of cerebral vascular diseasesd angina pectoris. |
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Uses |
Cardio-cerebral vascular medicine, used to improve the symptoms of ischemic cerebrovascular disease caused by cerebral vasospasm after subarachnoid hemorrhage |
This is an effective Rho kinase inhibitor and vasodilator. It also has inhibitory activity on PKA, PKG, PKC and MLCK.
Pharmacological action
Fasudil hydrochloride is an isoquinoline sulfonamide derivative, which can not only inhibit the activity of free calcium ions in cells, but also inhibit the protein kinase AGC and myosin light chain kinase, that is, inhibit smooth muscle contraction, the final stage of myosin Phosphorylation of light chain makes vascular smooth muscle relax and expand blood vessels. In vitro experiments show that this product can relax the isolated cerebral blood vessels, inhibit the isolated blood vessel contraction caused by the inflow of calcium ions Chemicalbook, can inhibit the contraction of various brain vasoconstrictor drugs with different mechanisms, and inhibit intracellular calcium ions. It has the effect of causing vasoconstriction, but does not reduce the intracellular calcium ion concentration and inhibits the production of myosin light chain phosphate during vasoconstriction. It is clinically used to improve and prevent cerebral vasospasm after subarachnoid hemorrhage and subsequent cerebral ischemia symptoms.
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