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.

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.

Orotirelin(CG 3509), a thyrotropin-releasing hormone analog, reversed pentobarbital-induced sleep time.Orotirelin may be beneficial in animals with focal cerebral ischemia.

Posatirelin (BRN6006446) is a synthetic peptide with modulatory activity and neurotrophic effects on monoaminergic and cholinergic systems for the study of vascular dementia.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

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.

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

Octinoxate (Octyl 4-methoxycinnamate) is used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage,primarily as an ingredient in some sunscreens and lip balms. It is also used to reduce the appearance of scars.

Iopanoic acid is an iodine contrast agent and a 5'-Deiodinase inhibitor.

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.

MB-07344 is a selective THR-β (thyroid hormone receptor β) agonist with a Ki of 2.17 nM, capable of reducing plasma total cholesterol (TPC) in both combination and monotherapy settings.

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.