β3-AR agonist 1

β3-AR agonist 1 (compound 15) 是一种高效选择性的，可口服的 β3-肾上腺素能受体 (β3-AR) 激动剂 (EC50=18 nM)，对 β1-、β2-、α1A-AR 无活性 (β1/β3, β2/β3, α1A/β3>556倍)。

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100mg

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250mg

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500mg

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Background

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.