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Thyroid Hormone Receptor Antagonist (1-850) (CAS 251310-57-3) LS-H132

Thyroid hormone receptor antagonist
LS-H132-1 / 1 mg / $185
LS-H132-5 / 5 mg / $255
LS-H132-10 / 10 mg / $335
USA Shipment Only
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Description: The activity of the thyroid hormones, L-thyroxine (T4) and 3,3',5-triiodo-L-thyronine (T3), is mediated by thyroid hormone nuclear receptors TR alpha and TR beta . Gene knockout studies in mice indicate that TR alpha modulates the effect of thyroid hormone on calorigenesis and on the cardiovascular system, while TR beta plays a role in the development of the auditory system and in the negative feedback of thyroid stimulating hormone by T3 in the pituitary. Thyroid hormone receptor antagonist (1-850) competitively blocks T3 binding to both TR alpha and TR beta (IC50s = 1.5 µM), demonstrating ~1,000-fold lower affinity for TR alpha in intact cells compared with T3. This compound is specific, showing no effect on the activity of the related retinoic acid receptor alpha. H132_ChemicalStructureImage.png
2-[1-(4-nitrophenyl)-4-piperidinylidene]-acetic acid-2-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]hydrazide
 
biochemical, chemical, antagonist
LS-H132
251310-57-3
C21H20F3N5O4
≥98%
A crystalline solid
 
O=C(NNC(/C=C1CCN(C2=CC=C([N+]([O-])=O)C=C2)CC/1)=O)NC3=CC(C(F)(F)F)=CC=C3
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)
CZMAYVNXNKBQKX-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: THRA / THR Alpha related products

Usage Information

Thyroid hormone receptor antagonist (1-850) is supplied as a crystalline solid. A stock solution may be made by dissolving the thyroid hormone receptor antagonist (1-850) in the solvent of choice. Thyroid hormone receptor antagonist (1-850) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of thyroid hormone receptor antagonist (1-850) in ethanol is approximately 0.5 mg/ml and approximately 50 mg/ml in DMSO and DMF. Thyroid hormone receptor antagonist (1-850) is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, thyroid hormone receptor antagonist (1-850) should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. Thyroid hormone receptor antagonist (1-850) has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. O’Shea, P.J. and Williams, G.R. Insight into the physiological actions of thyroid hormone receptors from genetically modified mice. J. Endocrinol. 175(3), 553-570 (2002).
  2. Schapira, M., Raaka, B.M., Das, S., et al. Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking. Proc. Natl. Acad. Sci. USA 100(12), 7354-7359 (2003).

 


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