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Submit ReviewSB 772077B dihydrochloride
Description: Potent Rho-kinase inhibitor; vasodilator
Chemical Name: (3S)-1-[[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl]carbonyl]-3-pyrrolidinamine dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for SB 772077B dihydrochloride
SB 772077B dihydrochloride is a 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 for SB 772077B dihydrochloride
SB 772077B dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for SB 772077B dihydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 772077B dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 41.53 | 100 | |
| DMSO | 41.53 | 100 |
Preparing Stock Solutions for SB 772077B dihydrochloride
The following data is based on the product molecular weight 415.28. 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 | 2.41 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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Product Datasheets for SB 772077B dihydrochloride
References for SB 772077B dihydrochloride
References are publications that support the biological activity of the product.
Doe et al (2007) Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J.Pharmacol.Exp.Ther. 320 89 PMID: 17018693
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
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Keywords: SB 772077B dihydrochloride, SB 772077B dihydrochloride supplier, SB772077B, 2HCl, Rho, Kinase, inhibitors, inhibits, ROCK, anti-inflammatory, vasodilators, antihypertensive, Rho-kinases, 4118, Tocris Bioscience
1 Citation for SB 772077B dihydrochloride
Citations are publications that use Tocris products. Selected citations for SB 772077B dihydrochloride include:
Lotz-Jenne et al (2016) A high-content EMT screen identifies multiple receptor tyrosine kinase inhibitors with activity on TGFβ receptor. Oncotarget 7 25983 PMID: 27036020
Do you know of a great paper that uses SB 772077B dihydrochloride from Tocris? Please let us know.
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Literature in this Area
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