H 1152 dihydrochloride

Cat. No. 2414

H 1152 dihydrochloride C16H21N3O2S.2HCl [871543-07-6]

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Chemical Name: (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride

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
Solubility:
Soluble to 100 mM in water and to 50 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
871543-07-6

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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

References

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.

Tamura et al (2005) Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 1754 245. PMID: 16213195.

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.

If you know of a relevant citation for this product please let us know.

Keywords: H 1152 dihydrochloride, supplier, Selective, Rho-kinase, ROCK, inhibitors, Rho-Kinase, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, H1152, dihydrochloride

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