Biological Activity
Potent Rho-kinase (ROCK) inhibitor (IC50 value of approximately 5.6 nM at recombinant human ROCK1 and 2). Decreases pulmonary and systemic arterial blood pressures and increases cardiac output. Exhibits vasodilator activity that is more potent than Y-27632 (Cat.No 1254) or Fasudil (Cat.No. 0541).
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
Compound Libraries
SB 772077B dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 415.28 |
| Formula | C15H18N8O2.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 607373-46-6 |
| PubChem ID | 69157798 |
| InChI Key | HSROPTGRSYJPJY-JZGIKJSDSA-N |
| Smiles | NC1=NON=C1C3=NC2=CN=CC(C(N4CC[C@H](N)C4)=O)=C2N3CC.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 | 41.53 | 100 | |
| water | 41.53 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 415.28. 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 | 2.41 mL | 12.04 mL | 24.08 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.82 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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References
References are publications that support the products' biological activity.
Doe et al (2007) Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J.Pharm.Exp.Ther. 320 89 PMID:
Dhaliwal et al (2009) Analysis of pulmonary vasodilator responses to SB-772077-B [4-(7-((3-amino-1-pyrrolidinyl)carbonyl)-1-ethyl-1H-imidazo(4,5-c)pyridin-2-yl)-1,2,5-oxadiazol-3-amine], a novel aminofurazan-based Rho kinase inhibitor. J.Pharm.Exp.Ther. 330 334 PMID:
Keywords: SB 772077B dihydrochloride, supplier, SB772077B, 2HCl, Rho, Kinase, inhibitors, inhibits, ROCK, anti-inflammatory, vasodilators, antihypertensive, Rho-kinases, Rho-kinases, Tocris Bioscience
