Biological Activity
Selective antagonist of adenosine A2B receptors (Ki values are 22, 1070, 1940 and 3280 nM for human A2B, A3, A1 and A2A receptors respectively). Attenuates allergen-, NECA- and AMP-induced airway reactivity in an allergic mouse model of asthma. Also shown to attenuate the inflammatory response during acute myocardial infarction in mice; reduces caspase-1 activity in the heart.
Technical Data
| M. Wt | 446.43 |
| Formula | C21H21F3N6O2 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 752222-83-6 |
| PubChem ID | 11270783 |
| InChI Key | KOYXXLLNCXWUNF-UHFFFAOYSA-N |
| Smiles | O=C(N(CC)C2=C1NC(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)=N2)N(CCC)C1=O |
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 | 2.23 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 446.43. 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 | 2.24 mL | 11.2 mL | 22.4 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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References
References are publications that support the products' biological activity.
Elzein et al (2008) Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J.Med.Chem. 51 2267 PMID: 18321039
Toldo et al (2012) GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J.Pharmacol.Exp.Ther. 343 587 PMID: 22923737
Mustafa et al (2007) Effect of a specific and selective A2B adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. J.Pharmacol.Exp.Ther. 320 1246 PMID: 17159162
Keywords: GS 6201, supplier, GS6201, CVT6883, asthma, adenosine, A2B, antagonists, allergy, antiallergics, selective, CVT, 6883, Adenosine, A2B, Receptors, Adenosine, A2B, Receptors, Tocris Bioscience
