Fasudil hydrochloride

Category	Human immunodeficiency Virus (HIV)
CAS	105628-07-7
Description	Fasudil HCl, a 5-isoquinolinesulfonamide derivative, is a highly selective Rho-associated protein kinase inhibitor that might have a rate in romoting the recovery of neurological function, reducing clinical symptoms and the morbidity.

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Product Information

Synonyms	Fasudil HCl; Eril; Fasudil (Hydrochloride); Fasudil Monohydrochloride; AT-877; HA-1077; AT 877; HA 1077; AT877; HA1077
IUPAC Name	5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride
Molecular Weight	327.83
Molecular Formula	C14H18ClN3O2S
Canonical SMILES	C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3
InChI	InChI=1S/C14H17N3O2S/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
InChIKey	NGOGFTYYXHNFQH-UHFFFAOYSA-N
Boiling Point	506.2°C at 760 mmHg
Melting Point	222 °C(dec.)
Flash Point	259.9°C
Purity	>98%
Density	1.289g/cm3
Solubility	DMSO: 5 mg/mL Water: 65 mg/mL
Appearance	White Crystalline Solid
Application	Fasudil HCl, a 5-isoquinolinesulfonamide derivative, is a highly selective Rho-associated protein kinase inhibitor that might have a rate in romoting the recovery of neurological function, reducing clinical symptoms and the morbidity.
Shelf Life	As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Storage	-20°C Freeze
Complexity	421
Exact Mass	327.0808257
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.
PSA	7.68
Target	ROCK; Calcium Channel; Autophagy; PKA; PKC; HIV