Biological Activity
Rho-kinase (ROCK) inhibitor that displays high selectivity over other protein kinases (IC50 values are 0.012, 0.180, 0.360, 0.745, 3.03, 5.68 and 28.3 μM for ROCKII, CAMKII, PKG, Aurora A, PKA, PKC and MLCK respectively). Inhibits sulprostone-induced contractions in guinea pig aorta (IC50 = 190 nM) and displays proerectile effects in rats. Glycyl derivative available (Cat. No. 2485).
Technical Data
| M. Wt | 392.34 |
| Formula | C16H21N3O2S.2HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 871543-07-6 |
| PubChem ID | 11560225 |
| InChI Key | BFOPDSJOLUQULZ-GXKRWWSZSA-N |
| Smiles | CC1=CN=CC2=C1C(S(N3CCCNC[C@@H]3C)(=O)=O)=CC=C2.Cl.Cl |
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 | |||
| DMSO | 19.62 | 50 | |
| water | 39.23 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 392.34. 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 | 2.55 mL | 12.74 mL | 25.49 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Shum et al (2003) Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP3 receptor agonist. Br.J.Pharmacol. 139 1449 PMID: 12922932
Teixeira et al (2005) Proerectile effects of the rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine (H-1152) in the rat penis. J.Pharmacol.Exp.Ther. 315 155 PMID: 15976017
Tamura et al (2005) Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 1754 245 PMID: 16213195
Keywords: H 1152 dihydrochloride, supplier, Selective, Rho-kinase, ROCK, inhibitors, inhibits, Rho-Kinase, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, H1152, dihydrochloride, Rho-kinases, Rho-kinases, Tocris Bioscience
