Cat. No. 2009
Chemical Name: 4-(2,3,6,7-Tetrahydro-2,6-dioxo-1-p
Biological ActivityHighly selective, water-soluble, human A2B adenosine receptor antagonist. Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. Also selective versus rat A1 and A2A receptors (Ki values are 2200 and 24000 nM respectively). Produces potent analgesic effects in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358. PMID: 14563788.
Yan and Muller (2004) Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability. J.Med.Chem. 47 1031. PMID: 14761205.
Hayallah et al (2002) 1,8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. J.Med.Chem. 45 1500. PMID: 11906291.
Muller et al (1998) 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists. Bioorg.Med.Chem. 6 707. PMID: 9681137.
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Citations are publications that use Tocris products. Selected citations for PSB 1115 include:
Ning et al (2014) Excess adenosine A2B receptor signaling contributes to priapism through HIF-1α mediated reduction of PDE5 gene expression. FASEB J 28 2725. PMID: 24614760.
Iannone et al (2013) Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma. Neoplasia 15 1400. PMID: 24403862.
Hua et al (2011) IL-4 amplifies the pro-inflammatory effect of adenosine in human mast cells by changing expression levels of adenosine receptors. PLoS One 6 e24947. PMID: 21966389.
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Keywords: PSB 1115, supplier, Selective, human, A2B, receptors, antagonists, water-soluble, adenosines, PSB1115, Tocris Bioscience, A2B Receptor Antagonist products
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