| Identification | Back Directory | [Name]
β3-AR agonist 1 | [CAS]
1283125-73-4 | [Synonyms]
β3-AR agonist 1
β3-AR agonist 1
β3 AR agonist 1,β3AR agonist 1
Cyclobutanesulfonamide, N-[3-[(1R)-1-hydroxy-2-[[2-[(3-methyl-1H-indazol-6-yl)oxy]ethyl]amino]ethyl]phenyl]- | [Molecular Formula]
C22H28N4O4S | [MDL Number]
MFCD32174249 | [MOL File]
1283125-73-4.mol | [Molecular Weight]
444.55 |
| Hazard Information | Back Directory | [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].
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]. | [Uses]
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]. | [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. |
|
|