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10007955 CAY10498
2-phenyl-amino-N6-endo-norbornyladenine
(CAS 863202-33-9)
CAY10498 Workbook Links
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The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation.1 A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold selectivity over A1 and A2A adenosine receptors, respectively.1 CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells.2 However, no dedifferentiation effects or any connection between A3 AR antagonism and dedifferentiation have been demonstrated.
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1
Perreira, M., Jiang, J., Klutz, A.M., et al. “Reversine” and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem 48 4910-4918 (2005).
2
Chen, S., Zhang, Q., Wu, X., et al. Dedifferentiation of lineage-committed cells by a small molecule. J Am Chem Soc 126 410-411 (2004).
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Pricing updated 2010-03-20.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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