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Merck
CN

609315-M

Thyroid Hormone Receptor Antagonist, 1-850

The Thyroid Hormone Receptor Antagonist, 1-850, also referenced under CAS 251310-57-3, controls the biological activity of Thyroid Hormone Receptor. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonym(s):

Thyroid Hormone Receptor Antagonist, 1-850, TR Antagonist, 1-850, 2-(2-(-(4-Nitrophenyl)-4-piperidinylidene)acetyl-N-(3-(trifluoromethyl)phenyl)-1-hydrazine Carboxamide

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About This Item

Empirical Formula (Hill Notation):
C21H20F3N5O4
CAS Number:
251310-57-3
Molecular Weight:
463.41
UNSPSC Code:
12352200
MDL number:
MFCD00134034
NACRES:
NA.77

Key Documents

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assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 5 mg/mL

Quality Level

100

General description

A cell-permeable hydrazinyl-carboxamide compound that acts as a selective and high-affinity thyroid hormone receptor (TR) antagonist (IC50 = 1.5 µM in HeLa cells). Shown to block T3- (L-triiodothyronine) mediated interaction of TRα with NRC (nuclear receptor coactivator) and prevent the stimulation of gene expression. Exerts no effect on the retinoic acid receptor α (RARα) activity.
A cell-permeable, selective, high-affinity thyroid hormone receptor (TR) antagonist (IC50 = 1.5 µM in HeLa cells). Reported to block T3-L-triiodothyronine)-mediated interaction of TRα with nuclear receptor coactivator (NRC) and prevent stimulation of gene expression. Exhibits no antagonistic effects on retinoic acid receptor α (RARα) activity.

Biochem/physiol Actions

Primary Target
Thyroid Hormone Receptor
Target IC50: 1.5 µM as antagonist for thyroid hormone receptor (TR) in HeLa cells

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Schapira, M., et al. 2003. Proc. Natl. Acad. Sci. USA100, 7354.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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