Description: Highly potent and selective adenosine A3 receptor antagonist
Chemical Name:N-[2-(2-Furanyl)-8-propyl-8H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-yl]-N'-(4-methoxyphenyl)urea
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent adenosine A3 receptor competitive antagonist. Selective for human A3 receptors over human A1 and A2A receptors (Ki values are 0.29, 141 and 1197 nM respectively). Potently inhibits agonist-induced cyclic AMP elevation in resting T lymphocytes (IC50 = 5 nM).
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
21.17
50
Preparing Stock Solutions
The following data is based on the product molecular weight 432.44. 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
2.31 mL
11.56 mL
23.12 mL
5 mM
0.46 mL
2.31 mL
4.62 mL
10 mM
0.23 mL
1.16 mL
2.31 mL
50 mM
0.05 mL
0.23 mL
0.46 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Gessiet al (2004) Expression of A3 adenosine receptors in human lymphocytes: up-regulation in T cell activation. Mol.Pharmacol. 65 711 PMID: 14978250
Varaniet al (2010) Expression and functional role of adenosine receptors in regulating inflammatory responses in human synoviocytes. Br.J.Pharmacol. 160 101 PMID: 20331607
Baraldiet al (1999) Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists. J.Med.Chem. 42 4473 PMID: 10579811