thyroid hormone receptor

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.

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.

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

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

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.

Carbimazole (Athyromazole) is an Imidazolium thyroid antagonist, which is rapidly transformed into MMI in vivo and can be converted into methidazole in vitro, and can be used in the study of Graves' disease.

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

2-Thiouracil (Deracil) is a thiolated uracil derivative that is a known anti-hyperthyroid agent.

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.

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

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

DPC-AJ1951 acetate, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR). And characterized the activity of DPC-AJ1951 acetate in ex vivo and in vivo assays of bone resorption[1].

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

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

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.

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).

KAT681 is a liver selective thyromimetic.

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.

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.

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 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).

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