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:
Molecular Weight:
463.41
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
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
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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