A3AR modulator 1 (MRS8054) is an orally activeA3adenosine receptor(A3AR)(Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [³⁵S]GTPγS binding E_max^[1].

A3AR modulator 1 (compound 39) shows a few weak off-target interactions, with K_ivalues of 0.123 μM, 0.891 μM, and 2.6 μM for translocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively^[1].

In fasted Wistar rats, A3AR modulator 1 (compound 39) has considerably longer in vivo half-life and improved oral bioavailability (3.44 h, 64.0%F at 3 mg/kg; 3.84 h, 61.5%F at 10 mg/kg), indicating substantial oral bioavailability^[1].

484.38

C₂₃H₂₅IN₄

Room temperature in continental US; may vary elsewhere.

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