thyroid hormone receptor-β

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.

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

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.

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

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

MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB-07344, known for its cholesterol and triglycerides lowering activity and its function as a liver-targeted THR-β agonist.

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

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

MLS000389544 is a selective and potent thyroid hormone receptor β (TRβ) antagonist with a methylsulfonyl nitrobenzoic acid structure. It effectively inhibits the interaction between TRβ and steroid receptor coactivator 2 (SRC2).

ZTA-261 is a highly selective and low-toxicity agonist for the thyroid hormone receptor subtype β (THR-β), with an IC50 of 6.3 nM. It operates through the Liothyronine-mediated pathway to reduce body weight and visceral fat. This compound has applications in the study of lipid metabolism and obesity.

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].

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].

Sob-AM2 is an effective substrate targeting the fatty acid amide hydrolase (FAAH) expressed in the brain, with a Km of 1.3 μM. It delivers higher concentrations of Sobetirome to the central nervous system at minimal peripheral systemic doses, thereby activating the central thyroid hormone receptor β (TRβ).

ALG-055009, a thyroid hormone receptor β (THR-β) agonist, exhibits an EC50 of 0.063 μM. It has been shown to reduce total cholesterol levels in rats fed a high-fat diet. ALG-055009 is used in the study of fatty liver diseases associated with metabolic dysfunction.

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].