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A xanthin derivative that acts as a potent agonist of adenosine A2A receptors (Ki = 27 nM). Exhibits reduced affinity for A2B receptors (Ki = 67 nM), but offers greater selectivity over A1R (Ki = 290 nM) and A3R (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.
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.
Adenosine A2A Receptor Agonist I, CGS 21680, Hydrochloride - CAS 124182-57-6 - Calbiochem 分析证书
标题
批号
119137
参考
参考信息概述
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.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
A xanthin derivative that acts as a potent agonist of adenosine A2A receptors (Ki = 27 nM). Exhibits reduced affinity for A2B receptors (Ki = 67 nM), but offers greater selectivity over A1R (Ki = 290 nM) and A3R (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.
Form
White solid
Formulation
Supplied as a hydrochloride salt.
Intert gas (Yes/No)
Packaged under inert gas
CAS number
124182-57-6
Chemical formula
C₂₃H₂₉N₇O₆ • HCl
Structure formula
Purity
≥96% by HPLC
Solubility
DMSO (100 mM)
Storage
Protect from light
-20°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
