Thyroid Hormone Receptor

Compound 3, also known as Thyroid hormone receptor beta agonist-1, functions as a thyroid beta-agonist [1].

Resmetirom (VIA-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist.

PCO371 (2,4-Imidazolidinedione, 1-(3,5-dimethyl-4-(2-((4-oxo-2-(4-(trifluoromethoxy)phenyl)-1,3,8-triazaspiro(4.5)dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-5,5-dimethyl-) is an orally active full agonist of parathyroid hormone receptor 1. It has no effect on PTH type 2 receptor.

Liothyronine (Tresitope) is an active form of thyroid hormone, binding to β1 thyroid hormone receptor (TRβ1), and activates its activity.

Tiratricol (3,3',5-Triiodothyroacetic acid) is a metabolite of T3 and T4 thyroid hormones; promoted for hyperlipidemia, localized lipodystrophy, and obesity. Tiratricol has been used in trials studying the treatment of Allan-Herndon-Dudley Syndrome.

Liothyronine Sodium is the sodium salt form of liothyronine, a synthetic form of the levorotatory isomer of the naturally occurring thyroid hormone triiodothyronine (T3). Liothyronine sodium (3,3',5-Triiodo-L-thyronine sodium) binds to nuclear thyroid receptors which then bind to thyroid hormone response elements of target genes. As a result, liothyronine sodium induces gene expression that is required for normal growth and development. Liothyronine sodium is more potent and has a more rapid action than thyroxine (T4).

L-Thyroxine sodium (LT4 sodium), the major hormone derived from the thyroid gland, is the agonist of Thyroid hormone receptor alpha and beta.

2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE is targets the thyroid stimulating hormone receptor (human)

L-Thyroxine (NSC 36397) is the major hormone derived from the thyroid gland. L-Thyroxine (NSC 36397) is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. L-Thyroxine (NSC 36397) is released from thyroglobulin by proteolysis and secreted into the blood. L-Thyroxine (NSC 36397) is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.

Triiodothyronine Sulfate is a prodrug to the Conventional Hormone Therapy of Hypothyroidism. Triiodothyronine sulfate is the main metabolite of thyroid hormone triiodothyronine (T3). Triiodothyronine is an active form of thyroid hormone bind to β1 thyroid

ML-109 is a potent agonist of thyroid stimulating hormone receptor (TSHR) (EC50 of 40 nM)

NH-3 is a potent orally active thyroid hormone receptor (THR) antagonist which exhibits reversible behavior, demonstrated by an IC 50 of 55 nM. Derived from the selective thyromi-metic GC-1, NH-3 effectively inhibits the binding of thyroid hormones to their respective receptors, resulting in hindered cofactor recruitment.

Taltirelin acetate (TA-0910 acetate) is a superagonist of the thyrotropin-releasing hormone receptor (TRH-R), with an IC50 of 910 nM and an EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).

NCGC00229600 is an allosteric inverse thyrotropin receptor (TSHR) agonist. NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously and can be used in Graves' disease studies.

D3-βArr (NCGC00379308) is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 (EC50: 11.6 μM) by direct TSHR activation.

Eprotirome (KB2115), a synthetic thyroid hormone mimetic, is a thyroid hormone receptor agonist.

Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).

KB-141 is an agonist of thyroid hormone receptor.

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

3-Iodothyronamine is derived from the deiodination and decarboxylation of endogenous thyroxine. It activates the G protein-coupled receptor known as trace amine-associated receptor 1 at nanomolar concentrations whereupon it rapidly influences thyroid hormone actions including body temperature, heart rate, and cardiac output. It has also been reported to function in controlling lipid and glucose utilization, hormonal secretion, and neuronal function, and has been considered for use in chemically-induced hibernation for medical purposes.

Org41841 is an agonist of luteinising hormone/chorionic gonadotropin receptor and thyroid stimulating hormone receptor (EC50s: 0.2 and 7.7 μM, respectively) and can be used to study hyperthyroidism.

Taltirelin (TA-0910) is at thyrotropin-releasing hormone receptor (TRH-R) superagonist (IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release))[1].

GC 14 is a selective thyroid hormone receptor antagonist with IC50 values of 200 nM for hTRα and 35 nM for hTRβ.

Protirelin Acetate (TRH Acetate) is a thyrotropin-releasing hormone, stimulating the release of thyrotropin and prolactin from the anterior pituitary.

THRβ Agonist 1 is a potent and selective THRβ agonist. THRβ Agonist 1 has the potential to be used in studies of thyroid hormone receptor related disorders.

3,5-Diiodothyropropionic acid (C082182) is a thyroid hormone analog. It induces α-myosin heavy chain mRNA expression, binds to thyroid hormone receptor (Ka: 2.40 M and 4.06 M for TRα1 and TRβ1).

Compound 40, known as THR-β modulator-2, acts as a modulator for the thyroid hormone receptor β (THR-β) [1].

THR-β Modulator-1 (Compound 1a) is a potent modulator of the thyroid hormone receptor β, utilized in the study of thyroid hormone receptor-associated disorders [1].

N-Desbutyl dronedarone is an active metabolite of the antiarrhythmic agent dronedarone .1,2,3It is formed from dronedarone by cytochrome P450s (CYPs) and monoamine oxidase (MAO) in human hepatocyte preparations.4N-Desbutyl dronedarone inhibits the binding of 3,3’,5-triiodo-L-thyronine to the thyroid hormone receptors TRα1and TRβ1(IC50s = 59 and 280 μM for the chicken and human receptors, respectively).1It inhibits CYP2J2-mediated formation of 14,15-EET from arachidonic acid and soluble epoxide hydrolase-mediated formation of 14,15-DHET from 14,15-EET (IC50s = 1.59 and 2.73 μM, respectively, in cell-free assays).2N-Desbutyl dronedarone decreases intracellular ATP levels in H9c2 rat cardiomyocytes (IC50= 1.07 μM) and inhibits mitochondrial complex I, also known as NADH dehydrogenase, and mitochondrial complex II, also known as succinate dehydrogenase, activities in isolated rat heart mitochondria (IC50s = 11.94 and 24.54 μM, respectively).3 1.Van Beeren, H.C., Jong, W.M.C., Kaptein, E., et al.Dronerarone acts as a selective inhibitor of 3,5,3’-triiodothyronine binding to thyroid hormone receptor-α1: in vitro and in vivo evidenceEndocrinology144(2)552-558(2003) 2.Karkhanis, A., Tram, N.D.T., and Chan, E.C.Y.Effects of dronedarone, amiodarone and their active metabolites on sequential metabolism of arachidonic acid to epoxyeicosatrienoic and dihydroxyeicosatrienoic acidsBiochem. Pharmacol.146188-198(2017) 3.Karkhanis, A., Leow, J.W.H., Hagen, T., et al.Dronedarone-induced cardiac mitochondrial dysfunction and its mitigation by epoxyeicosatrienoic acidsToxicol. Sci.163(1)79-91(2018) 4.Klieber, S., Arabeyre-Fabre, C., Moliner, P., et al.Identification of metabolic pathways and enzyme systems involved in the in vitro human hepatic metabolism of dronedarone, a potent new oral antiarrhythmic drugPharmacol. Res. Perspec.2(3)e00044(2014)

AH-3960 is an thyroid hormone receptor-1 (PTHR1) agonist.

TRβ Agonist 1, a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, demonstrates an EC50 value of 21 nM. It is useful in the research of dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH) [1].

Protirelin (Thyroliberin) is a tripeptide that stimulates the release of thyrotropin and prolactin.

Calcitonin (8-32), salmon is a highly selective amylin receptor antagonist. Calcitonin, a hormone involved in calcium and phosphorus metabolism, is primarily produced by the parafollicular or C cells in the mammalian thyroid gland and is a 32 amino acid peptide cleaved from a larger prohormone.

Risarestat (CT-112) is a potent aldose reductase inhibitor and thyroid hormone receptor (TR) antagonist for the treatment of hypoglycemia.

Reverse T3 (3,3',5'-triiodo-L-thyronine) inhibits the increase of sodium current generated by other thyroid hormone analogs in neonatal rat myocytes.

TI17, an inhibitor of the thyroid hormone receptor-interacting protein Trip13, possesses anticancer activity by effectively inhibiting multiple myeloma (MM) cell proliferation and inducing cell cycle arrest and apoptosis. Trip13, an AAA-ATPase mediating double-strand break (DSB) repair, is inhibited by TI17, resulting in increased DNA damage [1].

MB-07344 sodium has additive cholesterol lowering activity in combination with Atorvastatin in rabbits, dogs and monkeys. MB-07344 sodium is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM.

THR-β Agonist 6, a selective and orally active compound targeting the thyroid hormone receptor β (THR-β), demonstrates specificity with EC50 values of 0.03 μM for THR-β and 0.22 μM for THR-α. This compound boasts a remarkable liver-to-serum ratio of 93:1 in mouse models, underscoring its efficacy and potential for research in nonalcoholic steatohepatitis (NASH) [1].

L-Thyroxine sodium salt pentahydrate, also known as Levothyroxine, is a synthetic hormone utilized in the study of hypothyroidism. It is biologically activated into Triiodothyronine (T3) from its original form, L-Thyroxine (T4), through conversion by DIO enzymes.