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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|water||7.77||20mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 350.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.85 mL||14.27 mL||28.54 mL|
|5 mM||0.57 mL||2.85 mL||5.71 mL|
|10 mM||0.29 mL||1.43 mL||2.85 mL|
|50 mM||0.06 mL||0.29 mL||0.57 mL|
References are publications that support the products' biological activity.
Muller et al (1998) 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists. Bioorg.Med.Chem. 6 707 PMID: 9681137
Hayallah et al (2002) 1,8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. J.Med.Chem. 45 1500 PMID: 11906291
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
If you know of a relevant reference for PSB 1115, please let us know.
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Keywords: PSB 1115, supplier, Selective, human, A2B, receptors, antagonists, water-soluble, adenosines, PSB1115, Adenosine, A2B, Receptors, Adenosine, A2B, Receptors, Tocris Bioscience
9 Citations for PSB 1115
Citations are publications that use Tocris products. Selected citations for PSB 1115 include:
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
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
Rao et al (2014) A dual role for autophagy in a murine model of lung cancer. Proc Natl Acad Sci U S A 5 3056 PMID: 24445999
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
Chia et al (2013) The protective effects of CD39 overexpression in multiple low-dose streptozotocin-induced diabetes in mice. J Clin Invest 62 2026 PMID: 23364452
Stagg et al (2010) Anti-CD73 antibody therapy inhibits breast tumor growth and metastasis. J Immunol 107 1547 PMID: 20080644
Hart et al (2009) Cutting Edge: A2B Adenosine receptor signaling provides potent protection during intestinal ischemia/reperfusion injury. Diabetes 182 3965 PMID: 19299692
Frick et al (2009) Contribution of adenosine A2B receptors to inflammatory parameters of experimental colitis. J Pharmacol Exp Ther 182 4957 PMID: 19342675
Eckle et al (2008) A2B adenosine receptor signaling attenuates acute lung injury by enhancing alveolar fluid clearance in mice. J Immunol 118 3301 PMID: 18787641
Do you know of a great paper that uses PSB 1115 from Tocris? If so please let us know.
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