tcsc0007741 LY377604

LY377604 is a human β₃-adrenergic receptor agonist with an EC₅₀ of 2.4 nM and also a β₁- and β₂-adrenergic receptor antagonist.

IC50 & Target: EC50: 2.4 nM (human β₃-adrenergic receptor)^[1]


β₁-adrenergic receptor, β₂-adrenergic receptor^[1]

In Vitro: LY377604 is a human β₃-adrenergic receptor agonist with an EC₅₀ of 2.4 nM and also a β₁- and β₂-adrenergic receptor antagonist. LY377604 causes a maximal increase in cyclic adenosine monophosphate (cAMP) levels, but does not stimulate cAMP accumulation in CHO cells transfected with either the human β₁ adrenergic receptor or the human β₂ adrenergic receptor^[1].

In Vivo: Administration of LY377604 to male Long-Evans rats fed a caloric dense diet results in stimulation of lipid utilization. This is observed as a decrease in respiratory quotient and persists for about 4 h before returning to that measured from vehicle-treated rats^[1].