Target: thyroid hormone receptor IC50: 1.5 μM Thyroid hormone receptor antagonist (1-850) was screened from a library of more than 250000 compounds as the antagonist of thyroid hormone receptor with the highest affinity. Thyroid Hormone Receptor Antagonist, 1-850 is a cell-permeable hydrazinyl-carboxamide compound which functions as a selective and high-affinity thyroid receptor antagonist with the IC50 value of 1.5 μM in Hela cells . The thyroid hormone receptor (TR) is a type of nuclear receptor that is activated by binding thyroid hormone, which plays a critical role in the regulation of metabolism and heart rate and the development of organisms. Thyroid hormone receptor antagonist (1-850) could competitively block T3 (L-triiodothyronine) binding to both TRα and TRβ, and suppress T3 mediated interaction of TRα with nuclear receptor coactivator (NRC) as well as prevent the stimulation of gene expression . In Vitro: no data available. In Vivo: no data available. Clinical trial: no data available.

Product information

CAS Number: 251310-57-3

Molecular Weight: 463.41

Formula: C21H20F3N5O4

Chemical Name: 2-[1-(4-nitrophenyl)piperidin-4-ylidene]-N-({[3-(trifluoromethyl)phenyl]carbamoyl}amino)acetamide

Smiles: [O-][N+](=O)C1C=CC(=CC=1)N1CCC(CC1)=CC(=O)NNC(=O)NC1C=CC=C(C=1)C(F)(F)F

InChiKey: CZMAYVNXNKBQKX-UHFFFAOYSA-N

InChi: InChI=1S/C21H20F3N5O4/c22-21(23,24)15-2-1-3-16(13-15)25-20(31)27-26-19(30)12-14-8-10-28(11-9-14)17-4-6-18(7-5-17)29(32)33/h1-7,12-13H,8-11H2,(H,26,30)(H2,25,27,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.