| Bioactivity | 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 Emax[1]. |
| Invitro | A3AR modulator 1 (compound 39) shows a few weak off-target interactions, with Ki values of 0.123 μM, 0.891 μM, and 2.6 μM for translocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively[1]. |
| In Vivo | 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]. |
| Name | A3AR modulator 1 |
| Formula | C23H25IN4 |
| Molar Mass | 484.38 |
| 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]. 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. |