TR antagonist 1

Modify Date: 2024-01-14 07:39:14

Use of 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.

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	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.

Molecular Formula	C₂₅H₂₃Br₂NO₄
Molecular Weight	561.26

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Price: ￥6791/10 mM * 1 mL in DMSO

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