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| | A3AR modulator 1 Basic information |
| | A3AR modulator 1 Chemical Properties |
| Boiling point | 628.1±50.0 °C(predicted) | | density | 1.482±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | | pka | 12.43±0.40(predicted) |
| | A3AR modulator 1 Usage And Synthesis |
| Uses | 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]. | | 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]. | | IC 50 | Adenosine A3 receptor | | References | [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. DOI:10.1021/acs.jmedchem.2c01170 |
| | A3AR modulator 1 Preparation Products And Raw materials |
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