Biological Activity
Cell-permeable active metabolite of Fasudil (HA 1077; Cat. No. 0541). Produces ATP-competitive and reversible inhibition of Rho-kinase and is ~ 100-fold selective over a range of other protein kinases. Inhibits neutrophil migration and produces potent vasodilatory effects in vivo.
Technical Data
| M. Wt | 343.83 |
| Formula | C14H17N3O3S.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 155558-32-0 |
| PubChem ID | 11371328 |
| InChI Key | XWWFOUVDVJGNNG-UHFFFAOYSA-N |
| Smiles | Cl.OC1=NC=CC2=C(C=CC=C12)S(=O)(=O)N1CCCNCC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 6.88 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 343.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.91 mL | 14.54 mL | 29.08 mL |
| 5 mM | 0.58 mL | 2.91 mL | 5.82 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.91 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Arai et al (1993) Inhibition by the protein kinase inhibitor HA1077 of the activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 46 1487 PMID: 8240400
Shimokawa et al (1999) Rho-kinase-mediated pathway induces enhanced myosin light chain phosphorylations in a swine model of coronary artery spasm. Cardiovasc.Res. 43 1029 PMID: 10615430
Utsunomiya et al (2001) Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. Br.J.Pharmacol. 134 1724 PMID: 11739249
Keywords: HA 1100 hydrochloride, supplier, Cell-permeable, selective, Rho-kinase, inhibitors, inhibits, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, Rho-Kinase, HA1100, hydrochloride, Hydroxyfasudil, Rho-kinases, Rho-kinases, Tocris Bioscience
