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Merck

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:
155558-32-0
Molecular Weight:
307.37 (free base basis)
MDL number:
MFCD06411567
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

Hydroxyfasudil, A cell-permeable, hydroxylated metabolite of HA 1077 that displays anti-anginal properties.

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

assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Harmful (C)

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.

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.

Packaging

Packaged under inert gas

Physical form

A 10 mM (2 mg/582 µl) solution in H₂O.

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

Storage Class

11 - Combustible Solids

wgk

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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Global Trade Item Number

SKUGTIN
390602-2MGCN04055977189995

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