PSB 1115

Catalog # Availability Size / Price Qty
2009/10
2009/50
PSB 1115 | CAS No. 152529-79-8 | Adenosine A2b Receptor Antagonists
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Description: Selective human A2B antagonist; water-soluble

Chemical Name: 4-(2,3,6,7-Tetrahydro-2,6-dioxo-1-propyl-1H-purin-8-yl)-benzenesulfonic acid

Purity: ≥98%

Product Details
Citations (10)
Supplemental Products
Reviews

Biological Activity

PSB 1115 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Contribution of adenosine A(2B) receptors in Clostridium difficile intoxication and infection.
    Warren, Cirle A, Li, Yuesheng, Calabrese, Gina M, Freire, Rosemayr, Zaja-Milatovic, Snjezana, van Opstal, Edward, Figler, Robert A, Linden, Joel, Guerrant, Richard
    Infect Immun, 2012;80(12):4463-73.
  2. Netrin-1 promotes diabetic corneal wound healing through molecular mechanisms mediated via the adenosine 2B receptor
    Y Zhang, P Chen, G Di, X Qi, Q Zhou, H Gao
    Sci Rep, 2018;8(1):5994.
  3. Antinociceptive effects of novel A2B adenosine receptor antagonists.
    Abo-Salem et al.
    J.Pharmacol.Exp.Ther., 2004;308:358
  4. 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists.
    Muller et al.
    Bioorg.Med.Chem., 1998;6:707
  5. 1,8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
    Hayallah et al.
    J.Med.Chem., 2002;45:1500
  6. 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

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Citations for PSB 1115

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

10 Citations: Showing 1 - 10

  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. Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation.
    Authors: Sassi Et al.
    J Clin Invest  2014;124:5385
  4. 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
  5. 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
  6. 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
  7. Anti-CD73 antibody therapy inhibits breast tumor growth and metastasis.
    Authors: Stagg Et al.
    J Immunol  2010;107:1547
  8. Contribution of adenosine A2B receptors to inflammatory parameters of experimental colitis.
    Authors: Frick Et al.
    J Pharmacol Exp Ther  2009;182:4957
  9. Cutting Edge: A2B Adenosine receptor signaling provides potent protection during intestinal ischemia/reperfusion injury.
    Authors: Hart Et al.
    Diabetes  2009;182:3965
  10. 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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