TR antagonist 1

Names

[ CAS No. ]:
500794-88-7

[ Name ]:
TR antagonist 1

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Others >> Thyroid Hormone Receptor
Research Areas >> Metabolic Disease

[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].

[References]

[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.


[Related Small Molecules]

liothyronine | MGL-3196 | Sobetirome | L-thyroxine | Tiratricol | eprotirome | Protirelin Acetate | KAT681 | PCO371

Chemical & Physical Properties

[ Molecular Formula ]:
C25H23Br2NO4

[ Molecular Weight ]:
561.26

Related Compounds