Catalog Number: 5428
Chemical Name: (1S,2R,3S,4R,5S)-4-[6-[[(3-Chlorophenyl)methyl]amino]-2-[2-(3,4-difluorophenyl)ethynyl]-9H-purin-9-yl]-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1-carboxamide
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:
  • Formula:
  • Solubility:
    Soluble to 10 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
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.
Background References
  1. Endogenous adenosine A3 receptor activation selectively alleviates persistent pain states.
    Little et al.
    Brain, 2015;138:28
  2. Structure-guided design of A3 adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
    Tosh et al.
    J.Med.Chem., 2012;55:4847
  3. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain.
    Tosh et al.
    Purinergic Signal., 2015;11:371
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