Biological Activity
High affinity and selective A3 adenosine receptor agonist (Ki ~ 3 nM); displays >1000-fold selectivity over A1 and A2A adenosine receptors. Reverses mechanoallodynia in several neuropathic pain models in vivo. Orally bioavailable.
Technical Data
| M. Wt | 564.97 |
| Formula | C28H23ClF2N6O3 |
| Storage | Store at -20°C |
| Purity | ≥96% (HPLC) |
| CAS Number | 1377273-00-1 |
| PubChem ID | 57523213 |
| InChI Key | LYLLLJJYBWLGHW-CIZVZKTGSA-N |
| Smiles | O=[C@](NC)[C@@]1(C2)[C@H]2[C@@H](N3C(N=C(C#CC6=CC(F)=C(F)C=C6)N=C4NCC5=CC(Cl)=CC=C5)=C4N=C3)[C@H](O)[C@@H]1O |
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 | 5.65 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 564.97. 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 | 1.77 mL | 8.85 mL | 17.7 mL |
| 5 mM | 0.35 mL | 1.77 mL | 3.54 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.77 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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References
References are publications that support the products' biological activity.
Little et al (2015) Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states. Brain 138 28 PMID: 25414036
Tosh et al (2012) Structure-guided design of A3 adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. J.Med.Chem. 55 4847 PMID: 22559880
Tosh et al (2015) Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 11 371 PMID: 26111639
Keywords: MRS 5698, supplier, High, affinity, selective, A3, adenosine, receptors, agonists, antinociceptive, MRS5698, Adenosine, A3, Receptors, Adenosine, A3, Receptors, Tocris Bioscience
