Catalog Number: 2009
Chemical Name: 4-(2,3,6,7-Tetrahydro-2,6-dioxo-1-propyl-1H-purin-8-yl)-benzenesulfonic acid
Biological Activity
Highly 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.
Technical Data
  • M.Wt:
    350.35
  • Formula:
    C14H14N4O5S
  • Solubility:
    Soluble to 100 mM in DMSO and to 20 mM in water with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at RT
  • CAS No:
    152529-79-8
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.
Background References
  1. Antinociceptive effects of novel A2B adenosine receptor antagonists.
    Abo-Salem et al.
    J.Pharmacol.Exp.Ther., 2004;308:358
  2. Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
    Yan and Muller
    J.Med.Chem., 2004;47:1031
  3. 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists.
    Muller et al.
    Bioorg.Med.Chem., 1998;6:707
  4. 1,8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
    Hayallah et al.
    J.Med.Chem., 2002;45:1500
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PSB 1115 include:

9 Citations: Showing 1 - 9
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  1. A dual role for autophagy in a murine model of lung cancer.
    Authors: Rao Et al.
    Proc Natl Acad Sci U S A 2014;5:3056
  2. Excess adenosine A2B receptor signaling contributes to priapism through HIF-1α mediated reduction of PDE5 gene expression.
    Authors: Ning Et al.
    FASEB J 2014;28:2725
  3. The protective effects of CD39 overexpression in multiple low-dose streptozotocin-induced diabetes in mice.
    Authors: Chia Et al.
    J Clin Invest 2013;62:2026
  4. Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma.
    Authors: Iannone Et al.
    Neoplasia 2013;15:1400
  5. IL-4 amplifies the pro-inflammatory effect of adenosine in human mast cells by changing expression levels of adenosine receptors.
    Authors: Hua Et al.
    PLoS One 2011;6:e24947
  6. Anti-CD73 antibody therapy inhibits breast tumor growth and metastasis.
    Authors: Stagg Et al.
    J Immunol 2010;107:1547
  7. Contribution of adenosine A2B receptors to inflammatory parameters of experimental colitis.
    Authors: Frick Et al.
    J Pharmacol Exp Ther 2009;182:4957
  8. Cutting Edge: A2B Adenosine receptor signaling provides potent protection during intestinal ischemia/reperfusion injury.
    Authors: Hart Et al.
    Diabetes 2009;182:3965
  9. A2B adenosine receptor signaling attenuates acute lung injury by enhancing alveolar fluid clearance in mice.
    Authors: Eckle Et al.
    J Immunol 2008;118:3301

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