251310-57-3

Basic information

• Product Name: THYROID HORMONE RECEPTOR ANTAGONIST, 1-850
• Synonyms: THYROID HORMONE RECEPTOR ANTAGONIST, 1-850;TR ANTAGONIST 1-850;2-(2-(-(4-NITROPHENYL)-4-PIPERIDINYLIDENE)ACETYL)-N-(3-(TRIFLUOROMETHYL) PHENYL)-1-HYDRAZINE CARBOXAMIDE;1-[[2-[1-(4-nitrophenyl)piperidin-4-ylidene]acetyl]amino]-3-[3-(trifluoromethyl)phenyl]urea
• CAS NO: 251310-57-3
• Molecular Formula: C21H20F3N5O4
• Molecular Weight: 463.41
• Mol File: 251310-57-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.464±0.06 g/cm3(Predicted)
• Solubility: ≤0.5mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide
• PKA: 9.75±0.43(Predicted)
• CAS DataBase Reference: THYROID HORMONE RECEPTOR ANTAGONIST, 1-850(CAS DataBase Reference)
• NIST Chemistry Reference: THYROID HORMONE RECEPTOR ANTAGONIST, 1-850(251310-57-3)
• EPA Substance Registry System: THYROID HORMONE RECEPTOR ANTAGONIST, 1-850(251310-57-3)

Safety Data

• Hazardous Substances Data: 251310-57-3(Hazardous Substances Data)

Usage

Description

THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 is a compound that specifically targets and blocks the binding of thyroid hormones, L-thyroxine (T4) and 3,3'',5-triiodo-L-thyronine (T3), to their respective nuclear receptors TRα and TRβ. This antagonist demonstrates a competitive inhibition with an IC50 of 1.5 μM for both receptors and shows a significantly lower affinity for TRα in intact cells compared to T3. It is a selective compound, as it does not affect the activity of the related retinoic acid receptor α.
Usage:
Used in Pharmaceutical Industry:
THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 is used as a therapeutic agent for conditions related to the dysregulation of thyroid hormone activity. By blocking the binding of T3 to TRα and TRβ, it can help modulate the effects of thyroid hormones on various physiological processes, such as calorigenesis, cardiovascular function, auditory system development, and the negative feedback of thyroid stimulating hormone in the pituitary.
Used in Research Applications:
In the field of scientific research, THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 serves as a valuable tool for studying the roles and interactions of thyroid hormone receptors TRα and TRβ in cellular processes and disease mechanisms. THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 can be utilized to investigate the specific functions of these receptors and their contribution to various physiological and pathological conditions.

target

thyroid hormone receptor

IC 50

1.5 μm

references

[1] schapira m, raaka b m, das s, et al. discovery of diverse thyroid hormone receptor antagonists by high-throughput docking[j]. proceedings of the national academy of sciences of the united states of america, 2003, 100(12): 7354-7359.