Date published: 2026-2-3

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

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Alternate Names:
TR Antagonist; 1-850, 2-(2-(-(4-Nitrophenyl)-4-piperidinylidene)acetyl-N-(3-(trifluoromethyl)phenyl)-1-hydrazine Carboxamide
Application:
Thyroid Hormone Receptor Antagonist, 1-850 is a selective and high-affinity thyroid hormone receptor (TR) antagonist
CAS Number:
251310-57-3
Purity:
≥95%
Molecular Weight:
463.42
Molecular Formula:
C21H20F3N5O4
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Thyroid Hormone Receptor Antagonist, 1-850 is a cell-permeable hydrazinyl-carboxamide compound which acts as a selective and high-affinity thyroid receptor antagonist (IC50 = 1.5 muM in HeLa cells). It is shown to block T3- (L-triiodothyronine) mediated interaction of TRalpha with nuclear receptor coactivator (NRC) as well as prevent the stimulation of gene expression. It exerts no effect on the retinoic acid receptor alpha (RARalpha) activity.


Thyroid Hormone Receptor Antagonist, 1-850 (CAS 251310-57-3) References

  1. Thyroid hormones induce activation of rat hepatic stellate cells through increased expression of p75 neurotrophin receptor and direct activation of Rho.  |  Zvibel, I., et al. 2010. Lab Invest. 90: 674-84. PMID: 20231820
  2. Regulation of early spontaneous network activity and GABAergic neurons development by thyroid hormone.  |  Westerholz, S., et al. 2010. Neuroscience. 168: 573-89. PMID: 20338226
  3. 3,5-di-iodothyronine stimulates tilapia growth through an alternate isoform of thyroid hormone receptor β1.  |  Navarrete-Ramírez, P., et al. 2014. J Mol Endocrinol. 52: 1-9. PMID: 24031088
  4. Thyroid hormone response element half-site organization and its effect on thyroid hormone mediated transcription.  |  Paquette, MA., et al. 2014. PLoS One. 9: e101155. PMID: 24971931
  5. L-thyroxine promotes a proliferative airway smooth muscle phenotype in the presence of TGF-β1.  |  Dekkers, BG., et al. 2015. Am J Physiol Lung Cell Mol Physiol. 308: L301-6. PMID: 25480330
  6. Thyroid Hormone Receptors Predict Prognosis in BRCA1 Associated Breast Cancer in Opposing Ways.  |  Heublein, S., et al. 2015. PLoS One. 10: e0127072. PMID: 26029931
  7. Triiodothyronine regulates cell growth and survival in renal cell cancer.  |  Czarnecka, AM., et al. 2016. Int J Oncol. 49: 1666-78. PMID: 27632932
  8. Inhibition of thyroid hormone receptor locally in the retina is a therapeutic strategy for retinal degeneration.  |  Ma, H., et al. 2017. FASEB J. 31: 3425-3438. PMID: 28428265
  9. BDE-47 and BDE-85 stimulate insulin secretion in INS-1 832/13 pancreatic β-cells through the thyroid receptor and Akt.  |  Karandrea, S., et al. 2017. Environ Toxicol Pharmacol. 56: 29-34. PMID: 28869857
  10. Dioxin Exposure Alters Molecular and Morphological Responses to Thyroid Hormone in Xenopus laevis Cultured Cells and Prometamorphic Tadpoles.  |  Taft, JD., et al. 2018. Toxicol Sci. 161: 196-206. PMID: 29294139
  11. Finding the Right Fit: Highly Selective Binding by the Thyroid Hormone Receptor.  |  Schmidt, CW. 2020. Environ Health Perspect. 128: 64001. PMID: 32579035
  12. Thyroid Hormone Signaling in Embryonic Stem Cells: Crosstalk with the Retinoic Acid Pathway.  |  Fernández, M., et al. 2020. Int J Mol Sci. 21: PMID: 33255695
  13. Identification of thyroid hormone/thyroid hormone receptor interaction based on aptamer-assisted protein-induced fluorescence enhancement.  |  Song, J., et al. 2021. Biosens Bioelectron. 191: 113444. PMID: 34175646
  14. Bisphenol S disrupts opsins gene expression and impairs the light-sensing function via antagonizing TH-TRβ signaling pathway in zebrafish larvae.  |  Wei, S., et al. 2023. Food Chem Toxicol. 172: 113588. PMID: 36574878

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Thyroid Hormone Receptor Antagonist, 1-850, 1 mg

sc-222357A
1 mg
$77.00

Thyroid Hormone Receptor Antagonist, 1-850, 5 mg

sc-222357
5 mg
$96.00

Thyroid Hormone Receptor Antagonist, 1-850, 10 mg

sc-222357B
10 mg
$132.00

Does 1-850 dissolved in DMSO lose its activity even after repeated freeze-thaw cycles?

Asked by: Ryo01
Thank you for your question.It would be helpful if you could email us directly to asia@scbio.cn for more interactive discussions on this and other related issues.
Answered by: Zhanglong
Date published: 2024-05-08

It this compound at all soluble in sterile saline?

Asked by: maxinar
Thank you for your question. Unfortunately, we do not have any solubility data for this product in sterile saline.
Answered by: Tech Support Europe
Date published: 2020-08-25

Is this soluble in the storage condition after solving in DMSO? How long will it be stable?

Asked by: Io5ay
Thank you for your question. This chemical is soluble in DMSO at 5 mg/ml. Following reconstitution, store at -20ºC - stock solutions should be stable for up to 3 months. Please contact Technical Service if you have further questions concerning this product.
Answered by: Tech Service 9
Date published: 2021-08-26
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Rated 5 out of 5 by from DekkersDekkers, et al. (PubMed ID 25480330) treated ASM cells with 3 M of the specific thyroid receptor antagonist, 1-850 to determine which receptors may be involved together for proliferation between T4 and TGF- 1. -SCBT Publication Review
Date published: 2015-07-15
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Thyroid Hormone Receptor Antagonist, 1-850 | CAS 251310-57-3 is rated 5.0 out of 5 by 1.
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