Thyroid Hormone Receptor
THR
Thyroid hormone receptor is a member of the nuclear receptor superfamily that shuttles between the cytosol and nucleus. Thyroid hormone receptors are ligand-dependent transcription factors that mediate the biological activities of thyroid hormone (T3). Thyroid hormone receptors are encoded by two genes, one for TRα and another for TRβ, which encode the major isoforms of TR, including TRα1, TRα2, TRβ1, and TRβ2. The thyroid hormone receptors mediate the pleiotropic activities of the thyroid hormone (T3) in growth, development, and differentiation and in maintaining metabolic homeostasis.
Thyroid hormone receptors are zinc finger transcription factors in the erbA superfamily that bind DNA at specific response element sequences (thyroid hormone response elements, TREs) and activate gene expression in response to thyroid hormone (T3). Thyroid hormone receptors have been shown to bind DNA as monomers, homodimers, or heterodimers with another erbA superfamily member, the retinoid X receptor (RXR).
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Thyroid Hormone Receptor Inhibitors
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Thyroid Hormone Receptor Agonists
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Thyroid Hormone Receptor Antagonists
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Thyroid Hormone Receptor Modulators
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Thyroid Hormone Receptor Controls
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Thyroid Hormone Receptor Ligand
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Thyroid Hormone Receptor Related Products (188)
Related Products (188)
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Antibodies (5)
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Parathyroid hormone (1-34) (rat)
0 ImagesParathyroid hormone (1-34) (rat) is a parathyroid hormone. Parathyroid hormone (1-34) (rat) improves both cortical and cancellous bone structure. Parathyroid hormone (1-34) (rat) can be used for the research of osteoporosis.
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Protirelin acetate
0 ImagesSynonyms: Thyrotropin-releasing-hormone acetate; TRH acetateProtirelin Acetate is a highly conserved neuropeptide that exerts the hormonal control of thyroid-stimulating hormone (TSH) levels as well as neuromodulatory functions.
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Fenclofenac
0 ImagesSynonyms: Flenac; R 67408Fenclofenac is an orally active anti-inflammatory agent with a low ulcerogenic effect. Fenclofenac also exhibits antipyretic and analgesic activities, with an oral LD50 of 2280 mg/kg in rats. Fenclofenac can be utilized in inflammation research.
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Elunetirom
0 ImagesSynonyms: MA-JD21; ABX-002Elunetirom (MA-JD21) is an orally active, blood-brain barrier-permeable prodrug of LL-340001. Elunetirom employs fatty acid amide hydrolase (FAAH)-dependent prodrug technology to enhance the brain delivery of LL-340001, a potent thyroid hormone receptor agonist with 15-fold higher selectivity for TRβ over TRα. Elunetirom induces T3-regulated gene expression, including that of ABCD2. Elunetirom drives neuroplasticity and bioenergetic changes, and induces neurogenesis, neuritogenesis, and synaptogenesis. Elunetirom is applicable to research related to major depressive disorder and X-linked adrenoleukodystrophy.
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ALG-055009
0 ImagesCat. No.: HY-168046CAS No.: 2542029-03-6ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC50 of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease.
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Encaleret
0 ImagesSynonyms: CLTX-305; JTT-305; MK-5442Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.
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CO23
0 ImagesCO23 is a selective thyroid hormone receptor (TR) α agonist and used for growth and development regulation.
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TI17
0 ImagesCat. No.: HY-Q04764CAS No.: 1005178-02-8TI17 is an inhibitor of the thyroid hormone receptor-interacting protein Trip13 and has anticancer activity. TI17 effectively inhibits multiple myeloma (MM) cell proliferation and induces cell cycle arrest and apoptosis. Trip13 is an AAA-ATPase that mediates double-strand break (DSB) repair; TI17 inhibits Trip13 function and increases DNA damage.
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VK-0214
0 ImagesVK-0214 is an agonist of the thyroid β receptor (TRβ). By activating the expression of ABCD2, it can reduce the accumulation of very long-chain fatty acids (VLCFAs) and further alleviate glioblastoma multiforme. VK-0214 has the effect of regulating fatty acid metabolism and can be used in the research of X-linked adrenoleukodystrophy (X-ALD).
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TR antagonist 2
0 ImagesCat. No.: HY-127024ACAS No.: 1073179-55-1TR antagonist 2 (Compound 10a) is a competitive thyroid hormone receptors (TRα/β) antagonist (IC50=47 nM). TR antagonist 2 competes with triiodothyronine (T3) for binding to the ligand-binding domain of TR to block receptor-coactivator complex formation and inhibit target gene transcription, reducing thyroid hormone-mediated hypermetabolic effects. TR antagonist 2 is promising for research of hyperthyroidism (e.g., Graves' disease) and thyrotoxicosis.
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(Glu2)-TRH
0 Images(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS.
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Sob-AM2
0 ImagesSob-AM2 is a potent substrate (Km=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice.
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Debutyldronedarone hydrochloride
0 ImagesSynonyms: SR35021 hydrochlorideDebutyldronedarone hydrochloride (SR35021 hydrochloride) is a Cytochrome P450 enzyme inhibitor and a Thyroid Hormone Receptor inhibitor, and it is a metabolite of Dronedarone (HY-A0016). Debutyldronedarone hydrochloride inhibits the binding of T3 to TRα1 and TRβ1. Debutyldronedarone hydrochloride reduces the incidence of reperfusion-induced ventricular fibrillation in anesthetized rats, while decreasing their heart rate and blood pressure. Debutyldronedarone hydrochloride can be used in studies related to ventricular fibrillation and atrial fibrillation.
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Canvuparatide
0 ImagesCat. No.: HY-P10909CAS No.: 2925554-87-4Synonyms: MBX 2109Canvuparatide (MBX 2109) is a prodrug for parathyroid hormone (PTH) peptide that releases the bioactive PTH[1-32] peptide agonist that retains a fatty acylated lysine (Lys33) at the C-terminus, thereby extending the halflife of Canvuparatide. Canvuparatide can be used for the symptoms of hypoparathyroidism such as hypocalcemia and hyperphosphatemia.
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4,4'-Sulfonyldiphenol (Standard)
0 ImagesSynonyms: Bisphenol S (Standard); Bis(4-hydroxyphenyl) sulfone (Standard)4,4'-Sulfonyldiphenol (Bisphenol S; Bis(4-hydroxyphenyl) sulfone) (Standard) is the analytical standard of 4,4'-Sulfonyldiphenol (HY-W011927). This product is intended for research and analytical applications. 4,4'-Sulfonyldiphenol, a substitute for Bisphenol A (HY-18260), is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae.
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Taltirelin acetate
0 ImagesSynonyms: TA-0910 acetateTaltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca2+ concentration (Ca2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue.
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ZTA-261
0 ImagesZTA-261 is a highly selective and low toxic thyroid hormone receptor β subtype (THR-β) agonist (IC50=6.3 nM) that reduces body weight and visceral fat through a liothyronine (HY-A0070A) mediated pathway. ZTA-261 can be used in the study of lipid metabolism and obesity prevalence.
