Thyroid Hormone Receptor Antagon

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Thyroid Hormone Receptor Antagonist (1-850)

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Cat No: 17248

Biochemicals - Receptor Pharmacology

The activity of the thyroid hormones, L-thyroxine (T4; Item No. 14116) and 3,3',5-triiodo-L-thyronine (T3; Item No. 16028), is mediated by thyroid hormone nuclear receptors TRα and TRβ. Gene knockout studies in mice indicate that TRα modulates the effe...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

2-[1-(4-nitrophenyl)-4-piperidinylidene]-acetic acid-2-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]hydrazide

Correlated keywords:

1073179-55-1 hyperthyroidism nuclear receptor endocrinology antagonist obesity cardiology thyroid hormone TR biochemical block T3 L-thyroxine T4 3,3',5-triiodo-L-thyronine TR? TR? gene knockout calorigenesis cardiovascular system development auditory system negative feedback stimulating pituitary cell

Product Overview:
The activity of the thyroid hormones, L-thyroxine (T4; Item No. 14116) and 3,3',5-triiodo-L-thyronine (T3; Item No. 16028), is mediated by thyroid hormone nuclear receptors TRα and TRβ. Gene knockout studies in mice indicate that TRα modulates the effect of thyroid hormone on calorigenesis and on the cardiovascular system, while TRβ plays a role in the development of the auditory system and in the negative feedback of thyroid stimulating hormone by T3 in the pituitary.{22280} Thyroid hormone receptor antagonist (1-850) competitively blocks T3 binding to both TRα and TRβ (IC50s = 1.5 µM), demonstrating ~1,000-fold lower affinity for TRα in intact cells compared with T3.{28129} This compound is specific, showing no effect on the activity of the related retinoic acid receptor α.{28129}

Size	1 mg
Shipping	dry ice
CAS Number	251310-57-3
Molecular Formula	C₂₁H₂₀F₃N₅O₄
SMILES	O=C(NNC(/C=C1CCN(C2=CC=C([N+]([O-])=O)C=C2)CC/1)=O)NC3=CC(C(F)(F)F)=CC=C3
Molecular Weight	463,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.