PSB 11 hydrochloride
Potent and selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A1 and A2A receptors (Ki values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A1, rat A2A and mouse A2B receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 36 nM).
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||5.91||20mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 331.8. 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||3.01 mL||15.07 mL||30.14 mL|
|5 mM||0.6 mL||3.01 mL||6.03 mL|
|10 mM||0.3 mL||1.51 mL||3.01 mL|
|50 mM||0.06 mL||0.3 mL||0.6 mL|
References are publications that support the products' biological activity.
Muller et al (2002) Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A- and A3-adenosine receptor antagonists. J.Med.Chem. 45 3440 PMID: 12139454
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
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