General description

A xanthin derivative that acts as a potent agonist of adenosine A_2A receptors (K_i = 27 nM). Exhibits reduced affinity for A_2B receptors (K_i = 67 nM), but offers greater selectivity over A_1R (K_i = 290 nM) and A_3R (88.8 µM). Exerts an anti-inflammatory effect during chronic inflammation and ameliorates the tissue damage associated with collagen-induced arthritis. Also shown to reduce CCR7 Protein Expression in THP1 macrophages. Shown to delay the progressive deterioration of motor performance and prevent a reduction in brain weight in murine model of Huntington′s disease.

A xanthin derivative that acts as a potent agonist of adenosine A_2A receptors (K_i = 27 nM). Exhibits reduced affinity for A_2B receptors (K_i = 67 nM), but offers greater selectivity over A_1R (K_i = 290 nM) and A_3R (88.8 µM). Exerts an anti-inflammatory effect during chronic inflammation and ameliorates the tissue damage associated with collagen-induced arthritis. Also shown to reduce CCR7 Protein Expression in THP1 macrophages. Shown to delay the progressive deterioration of motor performance and prevent a reduction in brain weight in murine model of Huntington′s disease. Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Willians, A. J., et al. 2012. Inflammation.35, 614.Mazzon, E. et al. 2011. J Rheumatol.38, 2119,Martire, A., et al. 2007. Neurosci Lett.417, 78.Chou, S. Y., et al, 2005. Journ Neurochem.93, 310.Klotz, K. N., et al. 2000. Naunyn Schmiedebergs Arch Pharmacol.362 382.Phillis, J. W., et al. 1990.Brain Res.509, 328.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

Supplied as a hydrochloride salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)