
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
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Product NameTR antagonist 1
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NoteResearch use only, not for human use.
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Brief DescriptionTR 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.
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DescriptionTR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively.
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In VitroTR 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.
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In VivoTR 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.
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetTHR
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RecptorThyroid hormone receptor(THR)
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Research Area——
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Indication——
Chemical Information
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CAS Number500794-88-7
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Formula Weight561.26
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Molecular FormulaC25H23Br2NO4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 83.3 mg/mL (148.42 mM )
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SMILESCC(C)c1cc(Oc2c(Br)cc(CCC(O)=O)cc2Br)cc(\C=C\c2ccncc2)c1O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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