thyroid hormone receptor-β

Resmetirom (MGL-3196) is a THR-β agonist (EC50=0.21 μM), with high selectivity and oral activity. Resmetirom can be used in the research of non-cirrhotic and non-alcoholic steatohepatitis.

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.

Propylthiouracil (6-n-Propylthiouracil) is a thyroid peroxidase inhibitor and also a 5' -deiodinase inhibitor.

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 (Tresitope) is a synthetic and highly active thyroid hormone that acts as an effective agonist of TRα and TRβ (Ki = 2.33 nM for both hTRα and hTRβ). It activates the TRβ1 receptor, promotes the metabolism of carbohydrates, proteins, and fats, accelerates the oxidative processes in tissue cells, maintains basal metabolic rate, and supports normal growth and development. Liothyronine can be used to induce hyperthyroidism models.

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

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).

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.

L-Thyroxine sodium salt pentahydrate (Sodium levothyroxine pentahydrate) is a thyroid hormone with anticholesterol activity that inhibits the release of thyroid hormones from thyroid cancer nodules and is used in immune and endocrine disorders such as hypothyroidism, myxedema, cretinism and obesity. diseases, such as hypothyroidism, myxedema, cretinism and obesity.

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).

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.

Protirelin Acetate(24305-27-9 free base) (Thyroliberin Acetate) is a tripeptide that stimulates the release of thyrotropin and prolactin.

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) acetate is a highly potent antagonist of parathyroid hormone (PTH) The Ki value is 69 nM in bovine renal cortical membrane.

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.

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.

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.

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.

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).

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).

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

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].

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].

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].