HA-1077 (hydrochloride) structure
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Common Name | HA-1077 (hydrochloride) | ||
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CAS Number | 203911-27-7 | Molecular Weight | 382.306 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C14H21Cl2N3O3S | Melting Point | N/A | |
MSDS | Chinese USA | Flash Point | N/A |
Use of HA-1077 (hydrochloride)Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3]. |
Name | 1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride |
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Synonym | More Synonyms |
Description | Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3]. |
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Related Catalog | |
Target |
PKA:4.58 μM (IC50) PKC:12.3 μM (IC50) p160ROCK:0.33 μM (Ki) ROCK2:0.158 μM (IC50) PKG:1.65 μM (IC50) |
In Vitro | Fasudil dihydrochloride (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[4]. Fasudil dihydrochloride (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[4]. Fasudil dihydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4]. Western Blot Analysis[4] 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[4] 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. |
In Vivo | Fasudil dihydrochloride (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[5]. Fasudil dihydrochloride (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[6]. Fasudil dihydrochloride (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[6]. Animal Model: Myocardial ischemia and reperfusion in rat (250-300 g)[5] 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. |
References |
Molecular Formula | C14H21Cl2N3O3S |
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Molecular Weight | 382.306 |
Exact Mass | 381.068054 |
PSA | 79.91000 |
LogP | 4.10600 |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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RIDADR | NONH for all modes of transport |
RTECS | HM4031166 |
HS Code | 2942000000 |
HS Code | 2942000000 |
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Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase.
Br. J. Pharmacol. 98 , 1091, (1989) The in vitro and in vivo vasorelaxant effects of HA1077, 1-(5-isoquinolinesulphonyl)-homopiperazine HCl, a novel vasodilator were examined. The inhibitory effects of HA1077 on contractile responses to... |
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A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture.
J. Pharmacol. Exp. Ther. 259 , 738, (1991) The effects of a newly developed vasodilator agent, HA1077 [1-(5-isoquinolinesulfonyl)-homopiperazine hydrochloride], were investigated on the proliferation of cultured bovine aortic vascular smooth m... |
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Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle.
Eur. J. Pharmacol. 195 , 267, (1991) We examined the effects of HA1077, a potent inhibitor of protein kinases in vitro, on the relationship between tension and myosin-light chain (MLC20) phosphorylation in the initial phase of contractio... |
HA-1077 (hydrochloride) |
Fasudil dihydrochloride |
5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline dihydrochloride hydrate |
HA-1077 dihydrochloride |
Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride, hydrate (1:2:1) |
HA-1077 dihydrochloride,1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride,Fasudil dihydrochloride |