Biological Activity
Potent soluble guanylyl cyclase (sGC) inhibitor (Ki = 8 nM). Blocks sGC activity in murine cerebellum induced by S-nitroso-glutathione and NMDA (IC50 values are 17 and 20 nM respectively). Inhibits VEGF-induced cGMP accumulation; abolishes VEGF-induced migration in postcapillary venular endothelial cells (CVEC).
Technical Data
M. Wt | 269.05 |
Formula | C9H5BrN2O3 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 204326-43-2 |
PubChem ID | 4551 |
InChI Key | MUDRLQRJCGJJTB-UHFFFAOYSA-N |
Smiles | BrC1=CC=C(OCC(N23)=NOC3=O)C2=C1 |
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 | 26.91 | 100 | |
ethanol | 5.38 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 269.05. 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 | 3.72 mL | 18.58 mL | 37.17 mL |
5 mM | 0.74 mL | 3.72 mL | 7.43 mL |
10 mM | 0.37 mL | 1.86 mL | 3.72 mL |
50 mM | 0.07 mL | 0.37 mL | 0.74 mL |
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References
References are publications that support the products' biological activity.
von Wantoch Rekowski et al (2010) Synthesis and biological evaluation of oxadiazole derivatives as inhibitors of soluble guanylyl cyclase. Bioorg.Med.Chem. 18 1288 PMID: 20036129
Morbidelli et al (2010) The soluble guanylyl cyclase inhibitor NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability. Am.J.Physiol.Regul.Integr.Comp.Physiol. 298 R824 PMID: 20032260
Olesen et al (1998) Characterization of NS 2028 as a specific inhibitor of soluble guanylyl cyclase. Br.J.Pharmacol. 123 299 PMID: 9489619
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