β3-AR agonist 1

Names

[ Name ]:
β3-AR agonist 1

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

EC50: 18 nM (β3-AR)[1]

[In Vivo]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₈N₄O₄S

[ Molecular Weight ]:
444.55

β3-AR agonist 1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds