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
• Empirical Formula (Hill Notation): C₁₄H₁₇N₃O₃S · xHCl
• CAS Number: 155558-32-0
• Molecular Weight: 307.37 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Pictograms: GHS07
• Signal Word: Warning
• Hazard Statements: H302
• Precautionary Statements: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable