Thyroid hormone receptor(THR)

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.

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.

(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.

DS08210767 is a highly potent, orally bioavailable PTHR1 antagonist with an IC50 of 90 nM.

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

Azetirelin (YM 14673) is a new thyrotropin-releasing hormone (TRH) analog.

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

NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

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.

CO23 is a blood-brain barrier penetrant and selective TRα agonist and can be used in studies about the regulation of growth and development.

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.

3,5-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).

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.

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.

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).

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

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

Parathyroid Hormone (1-34), bovine, a parathyroid hormone (PTH) receptor agonist from the parathyroid hormone family, is used to study osteoporosis and hypoparathyroidism.

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

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

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

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

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.