产品
编 号：F762520
分子式：C23H25IN4
分子量：484.38
分子式：C23H25IN4
分子量：484.38
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CAS No: 2991693-62-8
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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 fortranslocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively.
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.
体内研究：
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.
体外研究：
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 fortranslocator protein (TSPO), opioid receptor σ2, and 5HT2B receptor, respectively.
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