Fasudil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fasudil Hydrochloride (INN) 是一种有效的 Rho 激酶抑制剂和血管扩张剂。

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.

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 AnalysisCell 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.

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.

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

Apoptosis

PKA

PKA| PKG| PKC| ROCK2| MLCK

Cancer

——

103745-39-7

291.37

C14H17N3O2S

>98% (HPLC)

Soluble in DMSO

O=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3)=O

1H-1,4-Diazepine, hexahydro-1-(5-isoquinolinylsulfonyl)-

(-20℃)

With Ice Pack

≥ 2 years