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
• Empirical Formula (Hill Notation): C₂₁H₂₀F₃N₅O₄
• CAS Number: 251310-57-3
• Molecular Weight: 463.41
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable