β3-AR agonist 1 |
カタログ番号GC37983 |
β3-AR アゴニスト 1 (化合物 15) は、非常に強力で選択的な経口利用可能な β3-アドレナリン受容体 (β3-AR) アゴニスト (EC50=18 nM) であり、β1-、β2-、および α1A- に対して不活性です。 AR (β1/β3、β2/β3、および α1A/β3 > 556 倍)。
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Cas No.: 1283125-73-4
Sample solution is provided at 25 µL, 10mM.
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold)[1]. EC50: 18 nM (β3-AR)[1]
β3-AR agonist 1 (compound 15) shows dose-dependent β3-AR-mediated responses in marmoset urinary bladder smooth muscle, has a desirable metabolic stability and pharmacokinetic profile (Cmax and AUC), and do not obviously affect heart rate or mean blood pressure when administered intravenously (3 mg/kg) to anesthetized rats[1].
[1]. Wada Y, et al. Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects. J Med Chem. 2017 Apr 27;60(8):3252-3265.
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