HA-1077 dihydrochloride

Category	Human immunodeficiency Virus (HIV)
CAS	203911-27-7
Description	HA-1077 is a potent and selective inhibitor of Rho kinase (ROCK). HA-1077 exhibited neuroprotective effects and enhanced cognition in mouse models of amyotrophic lateral sclerosis (ALS), suggesting its potential use for cognitive disorders such as ALS, Alzheimer's disease and spinal muscular atrophy. It also suppresses tumor cell motility and metastasis.

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Product Information

Synonyms	Fasudil dihydrochloride; 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline dihydrochloride
IUPAC Name	5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;dihydrochloride
Molecular Weight	364.3
Molecular Formula	C14H17N3O2S·2HCl
Canonical SMILES	C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl.Cl
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	NOXXIYDYFSNHDF-UHFFFAOYSA-N
Melting Point	>238°C (dec.)
Purity	≥98%
Solubility	In vitro: 10 mM in DMSO
Appearance	Crystalline Solid
Storage	Store at -20°C
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. 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. 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.
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. 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. 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.
PSA	79.91000
Target	PKA: 4.58 μM (IC50) PKC: 12.3 μM (IC50) PKG: 1.65 μM (IC50) p160ROCK: 0.33 μM (Ki) ROCK2: 0.158 μM (IC50)