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TR antagonist 1

CAS No. 500794-88-7

TR antagonist 1( —— )

Catalog No. M33185 CAS No. 500794-88-7

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    TR antagonist 1
  • Note
    Research use only, not for human use.
  • Brief Description
    TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.
  • 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.
  • 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.
  • 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.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    THR
  • Recptor
    Thyroid hormone receptor(THR)
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    500794-88-7
  • Formula Weight
    561.26
  • Molecular Formula
    C25H23Br2NO4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 83.3 mg/mL (148.42 mM )
  • SMILES
    CC(C)c1cc(Oc2c(Br)cc(CCC(O)=O)cc2Br)cc(\C=C\c2ccncc2)c1O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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