Fasudil Hydrochloride , 98% , 105628-07-7

Synonym(s):
1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride;Fasudil dihydrochloride

CAS NO.：105628-07-7

Empirical Formula: C14H18ClN3O2S

Molecular Weight: 327.83

MDL number: MFCD00943198

EINECS: 805-833-0

PRODUCT Properties

• Melting point: 220.5°; mp 219.3° (Shirotani)
• storage temp.: Inert atmosphere,Store in freezer, under -20°C
• solubility: H₂O: >200 mg/mL
• form: solid
• color: white
• Water Solubility: Soluble in water and dimethyl sulfoxide. Insoluble in ethanol.
• Merck: 14,3942
• 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.
• InChI: InChI=1S/C14H17N3O2S.2ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;;/h1,3-5,7,11,15H,2,6,8-10H2;2*1H
• InChIKey: LFVPBERIVUNMGV-UHFFFAOYSA-N
• SMILES: N1(S(C2=CC=CC3=C2C=CN=C3)(=O)=O)CCCNCC1.[H]Cl.[H]Cl

Description and Uses

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 diseases and angina pectoris.

Fasudil monohydrochloride is used in the prevention and treating cardiovascular and cerebrovascular diseases. It is also used in the inhibition of proliferation of vascular smooth muscle cells. It serves as a selective Rho-associated protein kinase (ROCK) inhibitor. Further, it protects against methyl mercury-induced axonal degeneration.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P264-P270-P301+P312+P330-P501-P301+P312a-P330-P501a
• Risk Statements: 22
• Safety Statements: 36-60
• WGK Germany: 3
• RTECS: HM4031166
• HS Code: 29339900
• Toxicity: LD50 in mice, rats (mg/kg): 67.5, 59.9 i.v.; 124.5, 123.2 s.c.; 273.9, 335.0 orally (Koga)