Debutyldronedarone

Debutyldronedarone (SR35021) inhibits the binding of T3 to human TRα₁ (K_i = 59 μM) and TRβ₁ (K_i = 280 μM) in vitro, with higher potency against the TRα₁ subtype; it also inhibits multiple human CYP isozymes in vitro, with K_i values ranging from 4.37 μM (CYP2D6) to 56.9 μM (CYP2B6)^[1].
Debutyldronedarone binds extensively to human plasma proteins (98.5%) and purified serum albumin (94.5-95.3%) in a non-saturable manner, whereas its binding to α₁-acid glycoprotein is saturable and concentration-dependent^[1].
Debutyldronedarone is metabolized by human CYP3A and CYP2D6 in vitro^[1].
Debutyldronedarone (DBDron) (10-100 μM) potently and competitively inhibits the binding of [¹²⁵I]T₃ to chicken TRα₁ with an IC₅₀ of 59 μM; meanwhile, it only exerts weak inhibitory effects on the binding of [¹²⁵I]T₃ to human TRβ₁, with an IC₅₀ of 280 μM, demonstrating TRα₁-selective antagonistic activity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.