PeptideDB

MRS5698

CAS: 1377273-00-1 F: C28H23ClF2N6O3 W: 564.97

MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human
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Bioactivity MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis[1][2].
Invitro MRS5698 displays higher affinity and selectivity (>3000-fold) agonist A3R vs. other adenosine receptor (ARs) in both human and mouse[1].MRS5698 (0.1-10 µM; 1 hours) induces a concentration-dependently robust A3R-mediated cAMP reduction in HEK-293T cells permanently expressing the A3R, regardless the illumination condition[3].
In Vivo MRS5698 (3 nmol/day; intrathecal injection for 25 days) prevents Oxaliplatin-induced mechano-allodynia and hyperalgesia, and attenuates Oxaliplatin-induced NLRP3/IL-1β neuroinflammation[2].MRS5698 (1 mg/kg; i.p. at days 2, 3 ) reduces the IL-23 induced (IL23 injected in day 0, 1, 3) ear thickness of C57BL/6N mouse during the third and fourth experimental days[3]. Animal Model:
Name MRS5698
CAS 1377273-00-1
Formula C28H23ClF2N6O3
Molar Mass 564.97
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [1]. Tosh DK, et al. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 2015;11(3):371-387. [2]. Wahlman C, et al. Chemotherapy-induced pain is promoted by enhanced spinal adenosine kinase levels through astrocyte-dependent mechanisms. Pain. 2018;159(6):1025-1034. [3]. López-Cano M, et al. Optical control of adenosine A3 receptor function in psoriasis. Pharmacol Res. 2021 Aug;170:105731.