MRS 5698 |
Catalog No.GC50162 |
MRS 5698 est un agoniste sélectif du récepteur de l'adénosine A3 couplé à la protéine Gi (A3AR), avec un Kis d'environ 3 nM pour l'A3AR humain et murin, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1377273-00-1
Sample solution is provided at 25 µL, 10mM.
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.
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
Average Rating: 5
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