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Fasudil

SKU: orb1941117

Description

Fasudil hydrochloride (INN) is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension.
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Images & Validation

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Fasudil

Key Properties

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CAS Number103745-39-7
MW291.37
Purity>98% (HPLC)
FormulaC14H17N3O2S
SMILESO=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3)=O
TargetPKA
SolubilitySoluble in DMSO

Bioactivity

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In Vivo
Fasudil (10 mg/kg; i. v. ; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio. Fasudil (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice. Animal model: Myocardial ischemia and reperfusion in rat (250-300 g). Dosage: 10 mg/kg. Administration: Intravenous injection; 1 h before operation. Result: Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus. Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.
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In Vitro
Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells. Fasudil (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells. Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells. Western blot analysis. Cell line: Rat HSCs and human HSC-derived TWNT-4 cells. Concentration: 50 μM; 100 μM. Incubation time: 24 hours. Result: Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%, and 90%, respectively. RT-PCR Cell line: Rat HSCs and human HSC-derived TWNT-4 cells. Concentration: 25 μM; 50 μM; 100 μM. Incubation time: 24 hours. Result: Reduced the expression of type I collagen, a-SMA, and TIMP-1.
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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Fasudil | AT 877 | AT-877 | AT877 | HA 1077

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Fasudil (orb1941117)

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