β3-AR agonist 1 |
| Katalog-Nr.GC37983 |
β3-AR-Agonist 1 (Verbindung 15) ist ein hochpotenter, selektiver und oral verfügbarer β3-adrenerger Rezeptor (β3-AR)-Agonist (EC50\u003d18 nM), der gegenüber β1-, β2- und α1A- inaktiv ist. AR (β1/β3, β2/β3 und α1A/β3 \u003e 556-fach).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1283125-73-4
Sample solution is provided at 25 µL, 10mM.
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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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