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
PSB 1115 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.84 | 100 | |
| 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 |
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Product Datasheets
References
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
Keywords: PSB 1115, supplier, Selective, human, A2B, receptors, antagonists, water-soluble, adenosines, PSB1115, Adenosine, A2B, Receptors, Adenosine, A2B, Receptors, Tocris Bioscience
