H 1152 dihydrochloride

Name: H 1152 dihydrochloride
Brand: Tocris Bioscience
SKU: 2414
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2414

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Citations (44)

COA / SDS

Selective Rho-kinase (ROCK) inhibitor

Key Product Details

Description:	Selective Rho-kinase (ROCK) inhibitor
Chemical Name:	(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	392.34

View Full Technical Details for H 1152 dihydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for H 1152 dihydrochloride

H 1152 dihydrochloride is a 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 also available.

Technical Data for H 1152 dihydrochloride

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for H 1152 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	39.23	100
	DMSO	19.62	50

Preparing Stock Solutions for H 1152 dihydrochloride

The following data is based on the product molecular weight 392.34.

Batch specific molecular weights may vary from batch to batch due to the degree 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	5.10 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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References for H 1152 dihydrochloride

References are publications that support the biological activity of the product.

Teixeira 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. 2005 PMID: 15976017
Tamura Development of specific Rho-kinase inhibitors and their clinical application. Biochim.Biophys.Acta 2005 PMID: 16213195
Shum Involvement of Rho-kinase in contraction of guinea-pig aorta induced by prostanoid EP₃ receptor agonist. Br.J.Pharmacol. 2003 PMID: 12922932