PSB 1115

Pricing Availability   Qty
Cat.No. 2009 - PSB 1115 | C14H14N4O5S | CAS No. 152529-79-8
Description: Selective human A2B receptor antagonist; water-soluble
Chemical Name: 4-(2,3,6,7-Tetrahydro-2,6-dioxo-1-propyl-1H-purin-8-yl)-benzenesulfonic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (10)
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 350.35
Formula C14H14N4O5S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 152529-79-8
PubChem ID 5311479
InChI Key UYDRRQPGDSIMNU-UHFFFAOYSA-N
Smiles O=C(NC2=C1NC(C3=CC=C(S(=O)(O)=O)C=C3)=N2)N(CCC)C1=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.84 100
water 7.77 20 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 the degree 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

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Product Datasheets

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References

References are publications that support the biological activity of the product.

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


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Keywords: PSB 1115, PSB 1115 supplier, Selective, human, A2B, receptors, antagonists, water-soluble, adenosines, PSB1115, Adenosine, Receptors, 2009, Tocris Bioscience

10 Citations for PSB 1115

Citations are publications that use Tocris products. Selected citations for PSB 1115 include:

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

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

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

Frick et al (2009) Contribution of adenosine A2B receptors to inflammatory parameters of experimental colitis. J Pharmacol Exp Ther 182 4957 PMID: 19342675

Hart et al (2009) Cutting Edge: A2B Adenosine receptor signaling provides potent protection during intestinal ischemia/reperfusion injury. Diabetes 182 3965 PMID: 19299692

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

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

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

Stagg et al (2010) Anti-CD73 antibody therapy inhibits breast tumor growth and metastasis. J Immunol 107 1547 PMID: 20080644

Sassi et al (2014) Cardiac myocyte-secreted cAMP exerts paracrine action via adenosine receptor activation. J Clin Invest 124 5385 PMID: 25401477


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