390602
Hydroxyfasudil
A cell-permeable, hydroxylated metabolite of HA 1077 that displays anti-anginal properties.
Synonym(s):
Hydroxyfasudil, ROCK Inhibitor XIV, 1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine, HCl, HA1100
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About This Item
Empirical Formula (Hill Notation):
C14H17N3O3S · xHCl
CAS Number:
Molecular Weight:
307.37 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
liquid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
assay
≥98% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
shipped in
wet ice
storage temp.
−20°C
SMILES string
[S](=O)(=O)(N3CCNCCC3)c1c2c([c]([nH]cc2)=O)ccc1.Cl
InChI
1S/C14H17N3O3S.ClH/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17;/h1,3-5,7,15H,2,6,8-10H2,(H,16,18);1H
InChI key
XWWFOUVDVJGNNG-UHFFFAOYSA-N
General description
A cell-permeable, hydroxylated metabolite of HA 1077 (Fasudil; Cat. No. 371970) that displays anti-anginal properties. Acts as an ATP-competitive and a reversible inhibitor of Rho-kinase (IC50 = 0.9 and 1.8 µM using a peptide and MLC as substrate, respectively) with ~100-fold greater selectivity over MLCK, MRCKβ, and PKC. Reported to inhibit the Rho kinase-mediated contraction both in vitro and in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Rho-kinase
Rho-kinase
Product competes with ATP.
Reversible: yes
Target IC50: 0.9 and 1.8 µM against Rho-kinase using a peptide and MLC as substrate, respectively
Packaging
Packaged under inert gas
Physical form
A 10 mM (2 mg/582 µl) solution in H₂O.
Other Notes
Ito, K., et al. 2003. J. Physiol.546, 823.
Takemoto, M., et al. 2002. Circulation106, 57.
Shimokawa, H., et al. 1999. Cardiovasc. Res.43, 1029.
Takemoto, M., et al. 2002. Circulation106, 57.
Shimokawa, H., et al. 1999. Cardiovasc. Res.43, 1029.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 390602-2MG | 04055977189995 |