tcsc0040844 TR antagonist 1

TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC₅₀s of 36 and 22 nM for TRα and TRβ, respectively.

IC50 & Target: IC50: 36 nM (Thyroid hormone α), 22 nM (Thyroid hormone α)^[1]

In Vitro: TR antagonist 1 displays high affinity for both thyroid hormone TRα and TRβ (IC₅₀=36 and 22 nM, respectively). TR antagonist 1 acts as a full antagonist in the TRAFR cell assay and the IC₅₀ 32 nM for both TRAFα1 and TRAFβ1^[1].

In Vivo: TR antagonist 1 treatment lowers heart rate and shows a possible trend toward an increase of low-density lipoprotein cholesterol (LDL-C) in the cholesterol fed rat model^[1].