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β3-AR agonist 1

Catalog No.GC37983

β L'agoniste 3-AR 1 (composé 15) est un agoniste des récepteurs β3-adrénergiques (β3-AR) très puissant, sélectif et disponible par voie orale (EC50 \u003d 18 nM), étant inactif pour β1-, β2- et α1A- AR (β1/β3, β2/β3 et α1A/β3\u003e 556 fois).

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β3-AR agonist 1 Chemical Structure

Cas No.: 1283125-73-4

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Description Chemical Properties Product Documents Related Products

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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