A3AR modulator 1 

A3AR modulator 1 (MRS8054) is an orally active A3 adenosine 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_i values of 0.123 μM, 0.891 μM, and 2.6 μM for translocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

484.38

C₂₃H₂₅IN₄

CCCC(C1=NC2=C(C3=C(N=C2NC4=CC=C(C=C4)I)C=CC=C3)N1)CCC

Room temperature in continental US; may vary elsewhere.

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

• [1]. Lucas B Fallot, e al. Structure-Activity Studies of 1 H-Imidazo[4,5- c]quinolin-4-amine Derivatives as A3 Adenosine Receptor Positive Allosteric Modulators. J Med Chem. 2022 Nov 24;65(22):15238-15262.  [Content Brief]