390602

Hydroxyfasudil

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

• Synonyme(s) : Hydroxyfasudil, ROCK Inhibitor XIV, 1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine, HCl, HA1100
• Formule empirique (notation de Hill) : C₁₄H₁₇N₃O₃S · xHCl
• Numéro CAS: 155558-32-0
• Poids moléculaire : 307.37 (free base basis)
• Numéro MDL: MFCD06411567
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Conditions d'expédition: wet ice
• Température de stockage: −20°C
• Chaîne SMILES: [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
• Clé InChI: XWWFOUVDVJGNNG-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Forme physique

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302
• Conseils de prudence: P264 - P270 - P301 + P312 - P501
• Classification des risques: Acute Tox. 4 Oral
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable