L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
