Potent, selective, competitive human A3 receptor antagonist
Potent, selective, competitive human A3 receptor antagonist (Ki values are 2.3 nM and 10 μM for human and rat A3 receptors, respectively), Antagonises human A1 and A2A receptors. Shows inverse agonist effects in the [35S]GTPγS binding assay. Shows anti-inflammatory effects.
Chemical name(R)-8-Ethyl-3,4,7,8-tetrahydro-4-methyl-2-phenyl-5H-imidazo[2,1-i]purin-5-one hydrochloride
Storage instructionsStore at -20°C. Store at -20°C long term. Store In the Dark. Store under Desiccating conditions. This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes.
Solubility overviewSoluble in DMSO to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Kim SK et al. Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor. J Mol Graph Model25:562-77 (2006).
Read more (PubMed: 16793299) »
Ozola V et al. 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 Chem11:347-56 (2003).
Read more (PubMed: 12517430) »
Müller CE et al. Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists. J Med Chem45:3440-50 (2002).
Read more (PubMed: 12139454) »
Gao ZG et al. Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives. Mol Pharmacol62:81-9 (2002).
Read more (PubMed: 12065758) »