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 hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM). Blocks the cytoprotective effect of A2A agonist CGS-21680 (Cat.No. 1063).
Technical Data
| M. Wt | 389.42 |
| Formula | C20H19N7O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 316173-57-6 |
| PubChem ID | 10668061 |
| InChI Key | AEULVFLPCJOBCE-UHFFFAOYSA-N |
| Smiles | COC1=CC=C(CCCN2N=CC3=C2N=C(N)N2N=C(N=C32)C2=CC=CO2)C=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 | 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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References
References are publications that support the products' biological activity.
Todde et 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
Zheng et 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:
Keywords: SCH 442416, supplier, selective, high, affinity, A2A, antagonists, Receptors, adenosines, SCH442416, adenosine, 2a, antagonist, Adenosine, A2A, Receptors, Adenosine, A2A, Receptors, Tocris Bioscience
