Biological Activity
Potent and highly selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1, A2A and A2B receptors (Ki values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A1 and A2A receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 4 nM). Produces thermal hyperalgesia in mice in vivo.
Technical Data
| M. Wt | 435.14 |
| Formula | C16H14Cl3N5O.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 591771-91-4 |
| PubChem ID | 90488733 |
| InChI Key | JUPMOTHIKGWECW-DDWIOCJRSA-N |
| Smiles | CC[C@H](C3)N=C1N3C(N(C)C2=C1NC(C4=C(Cl)C(Cl)=CC(Cl)=C4)=N2)=O.Cl |
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 | 10.88 | 25 | |
| ethanol | 4.35 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 435.14. 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 | 2.3 mL | 11.49 mL | 22.98 mL |
| 5 mM | 0.46 mL | 2.3 mL | 4.6 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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References
References are publications that support the products' biological activity.
Muller (2003) Medicinal chemistry of adenosine A3 receptor ligands. Curr.Top.Med.Chem. 3 445 PMID: 12570761
Ozola et al (2003) 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors. Bioorg.Med.Chem. 11 347 PMID: 12517430
Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358 PMID: 14563788
Keywords: PSB 10 hydrochloride, supplier, Potent, selective, human, A3, receptors, antagonists, inverse, agonists, adenosines, PSB10, hydrochloride, Adenosine, A3, Receptors, Adenosine, A3, Receptors, Tocris Bioscience
