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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).
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.62 mL||23.12 mL||46.25 mL|
|2.5 mM||0.92 mL||4.62 mL||9.25 mL|
|5 mM||0.46 mL||2.31 mL||4.62 mL|
|25 mM||0.09 mL||0.46 mL||0.92 mL|
References are publications that support the biological activity of the product.
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
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