500794-88-7

500794-88-7 structure
500794-88-7 structure
  • Name: TR antagonist 1
  • Chemical Name: TR antagonist 1
  • CAS Number: 500794-88-7
  • Molecular Formula: C25H23Br2NO4
  • Molecular Weight: 561.26
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2018-08-17 22:19:40
  • Modify Date: 2024-01-14 07:39:14
  • TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.

Name TR antagonist 1
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
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.

Molecular Formula C25H23Br2NO4
Molecular Weight 561.26