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390602

Sigma-Aldrich

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:
155558-32-0
Molecular Weight:
307.37 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

shipped in

wet ice

storage temp.

−20°C

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
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

Warning

Toxicity: Harmful (C)

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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