Description: Very selective, high affinity A2A antagonist
Chemical Name: 2-(2-Furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). Blocks the cytoprotective effect of A2A agonist CGS-21680 (Cat.No. 1063).
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
38.94
100
Preparing Stock Solutions
The following data is based on the product molecular weight 389.42. 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
2.57 mL
12.84 mL
25.68 mL
5 mM
0.51 mL
2.57 mL
5.14 mL
10 mM
0.26 mL
1.28 mL
2.57 mL
50 mM
0.05 mL
0.26 mL
0.51 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Toddeet al (2000) Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using positron emission tomography. J.Med.Chem. 43 4359 PMID: 11087559
Zhenget al (2007) Protective roles of adenosine A1, A2, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am.J.Physiol.Heart Circ.Physiol. 293 3685 PMID: