Biological Activity
Potent adenosine A3 receptor competitive antagonist. Selective for human A3 receptors over human A1 and A2A receptors (Ki values are 0.29, 141 and 1197 nM respectively). Potently inhibits agonist-induced cyclic AMP elevation in resting T lymphocytes (IC50 = 5 nM).
Technical Data
| M. Wt | 432.44 |
| Formula | C21H20N8O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 252979-43-4 |
| PubChem ID | 5310960 |
| InChI Key | CJRNHKSLHHWUAB-UHFFFAOYSA-N |
| Smiles | O=C(NC4=CC=C(OC)C=C4)NC2=NC1=NN(CCC)C=C1C3=NC(C5=CC=CO5)=NN23 |
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 | 21.17 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 432.44. 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 | 2.31 mL | 11.56 mL | 23.12 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.62 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Gessi et al (2004) Expression of A3 adenosine receptors in human lymphocytes: up-regulation in T cell activation. Mol.Pharmacol. 65 711 PMID: 14978250
Varani et al (2010) Expression and functional role of adenosine receptors in regulating inflammatory responses in human synoviocytes. Br.J.Pharmacol. 160 101 PMID: 20331607
Baraldi et al (1999) Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. J.Med.Chem. 42 4473 PMID: 10579811
Keywords: MRE 3008F20, supplier, adenosine, A3, receptors, potent, selective, competitive, antagonists, A3AR, MRE3008F20, hA3, Adenosine, A3, Receptors, Adenosine, A3, Receptors, Tocris Bioscience
