TRantagonist1是高亲和力的甲状腺激素受体(thyroidhormonereceptor(TR))拮抗剂，对TRα和TRβ的IC50值分别为36和22nM。
TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.
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].
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].
[1]. Koehler K, et al. Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem. 2006 Nov 16;49(23):6635-7.
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