Fasudil (HA-1077) hydrochloride

Research use only, not for human use.

Fasudil hydrochloride(HA-1077; AT-877) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK.

Fasudil hydrochloride(HA-1077; AT-877) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.(In Vitro):Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells. (In Vivo):Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (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.

Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (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 24 hours Incubation Time:24 hours Result:Reduced the expression of type I collagen, a-SMA, and TIMP-1.

Fasudil Hydrochloride (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 Hydrochloride (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 Hydrochloride (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.

HA-1077 | AT-877

Apoptosis

PKA

PKA| PKG| PKC| ROCK2| MLCK

Cancer

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105628-07-7

327.83

C14H18ClN3O2S

>98% (HPLC)

Water: 65 mg/mL (198.27 mM); DMSO: 5 mg/mL (15.25 mM)

Cl.Cl.O=S(=O)(N1CCCNCC1)C1=CC=CC2=C1C=CN=C2

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(-20℃)

With Ice Pack

≥ 2 years