thr-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.

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.

THR-β agonist 8 (Compound 1) is an orally active agonist for both TRα and TRβ. It holds potential for research into thyroid hormone-related diseases.

THR-β agonist 2 diacetate (Compound 3) is a potent THR-β agonist with potential applications in researching metabolic disorders such as obesity, hyperlipidemia, hypercholesterolemia, and diabetes, as well as other conditions like steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis, and other related diseases and conditions.

THR-β agonist 9 is a potent and selective THR-β activator, which shows sensitivity to His435 mutations with an EC50 of 3.2 nM. It demonstrates moderate selectivity, approximately 10-fold, and effectively activates various His435 mutants (H435A, H435Y, and H435R), with EC50 values ranging from 134.2 nM to 515.5 nM. THR-β agonist 9 presents potential for research into conditions such as dyslipidemia, metabolic syndrome-associated steatohepatitis (MASH), and resistance to thyroid hormone (RTH).

THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. It demonstrates robust cholesterol-lowering effects in cholesterol-fed rats. In a high-fat diet-carbon tetrachloride (HFD-CCl4) induced model of metabolic dysfunction-associated steatohepatitis (MASH) in mice, THR-β agonist 11 significantly reduces serum total triglycerides (TG), low-density lipoprotein cholesterol (LDL-cholesterol), liver total cholesterol (TC), and TG levels. Additionally, it alleviates hepatic steatosis, inflammation, and fibrosis. THR-β agonist 11 is applicable in the study of MASH and other fibrotic diseases.

THR-β agonist 10 is an orally active and selective THR-β agonist with an EC50 value of 11 nM. It effectively lowers levels of ALT (alanine aminotransferase), TC (total cholesterol), and LDL-C (low-density lipoprotein cholesterol). In mouse models of metabolic dysfunction-associated steatohepatitis (MASH), it improves steatosis, ballooning, inflammation, and fibrosis. THR-β agonist 10 is utilized in the research of MASH.

THR-β modulator-3 (Compound 75-2) is a THR-β modulator that reduces total body fat and weight, and improves obesity.

THR-β agonist 5 (compound 54) is a potent THR-β agonist with an EC50 of less than 50 nM [1].

THR-β agonist 2 is a potent agonist of THR-β with potential for studies of metabolic diseases (e.g., obesity, hyperlipidaemia, hypercholesterolaemia, diabetes, steatosis, non-alcoholic steatohepatitis [NASH], atherosclerosis, and other related conditions).

THR-β agonist 4 is a potent THR-β agonist with significant research potential for treating metabolic diseases such as hyperlipidemia, obesity, hypercholesterolemia, diabetes, steatosis, non-alcoholic steatohepatitis (NASH), and atherosclerosis, as well as other related conditions.

THR-β agonist 3 is a potent agonist of THR-β with demonstrated research potential for metabolic diseases, including obesity, hyperlipidemia, hypercholesterolemia, diabetes, steatosis, non-alcoholic steatohepatitis (NASH), and atherosclerosis.

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].

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

THRβ Agonist 1 is a potent and selective THRβ agonist. THRβ Agonist 1 has the potential to be used in studies of thyroid hormone receptor related disorders.

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.