Thyroid Hormone Receptor Agonist

Macotirom is a thyroid hormone β receptor agonist. Macotirom can be used in studies related to metabolic diseases and the liver.

THR-β agonist 8 (Compound 1) is an orally active agonist of TRα and TRβ. THR-β agonist 8 is promising for research of thyroid hormone-related diseases.

Prepro-TRH-(160-169) is one of the connecting peptides of thyrotropin-releasing hormone prohormone (pro-TRH), potentiates TRH-induced thyrotropin (TSH) release.

Etiroxate (CG-635) is a lipid lowing compound which can be used for hyperlipoproteinemia research.

THR-β agonist 2 (Compound 3) diacetate is a selective thyroid hormone receptor β (THRβ) agonist with an EC₅₀ of 1.42 μM. THR-β agonist 2 diacetate can regulate the biological pathways mediated by thyroid hormones. THR-β agonist 2 diacetate can be used for the study of metabolic diseases.

THR-β agonist 10 is an orally active and selective THR-β agonist, with an EC₅₀ of 11 nM. THR-β agonist 10 significantly reduces ALT (Alanine Aminotransferase), TC (Total Cholesterol), and LDL-C (Low-Density Lipoprotein Cholesterol) levels, and improves steatosis, ballooning, inflammation and fibrosis in the metabolic dysfunction-associated steatohepatitis (MASH) mouse model. THR-β agonist 10 can be used for the study of MASH.

TRβ agonist 2 (Compound 1) is a potent agonist of TRβ. TRβ agonist 2 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 2 is a new potential TRβ-selective thyromimetics.

THRβ receptor agonist-1 is a THRβ receptor agonist.

THR-β agonist-1 (Example 2) is a THR-β agonist, with EC₅₀ values of 52 nM and 1017 nM for THR-β and THR-α, respectively.

Resmetirom-¹³C₃,¹⁵N (MGL-3196-¹³C₃,¹⁵N) is the ¹³C- and ¹⁵N-labeled Resmetirom (HY-12216). Resmetirom (MGL-3196) is a highly selective and orally active thyroid hormone receptor β (THR-β) agonist with an EC₅₀ value of 0.21 μM. Resmetirom can be used for the study of noncirrhotic nonalcoholic steatohepatitis.

Taltirelin-¹³C,d₃ (TA-0910-¹³C,d₃) is ¹³C and deuterated labeled Taltirelin (HY-B0596). Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC₅₀ of 910 nM and EC₅₀ of 36 nM for stimulating an increase in cytosolic Ca²⁺ concentration (Ca²⁺ release).

PF-00277343 is a selective and skin-penetrable THR-β (K_i: 0.51 nM for THR-β, 8.0 nM for THR-α) agonist. PF-00277343 is effective against androgenetic alopecia in animal models.

Thyroid hormone receptor beta agonist-1 (compound 3) is a thyroid beta-agonist.

ZG-2585 is an orally active and selective thyroid hormone receptor β (THRβ) agonist. ZG-2585 selectively activates THRβ over THRα, driving allosteric conformational changes and coactivator recruitment. ZG-2585 reduces body weight, hepatic steatosis and lipid accumulation in a Western diet-induced metabolic disorder model. ZG-2585 can be used for the research of metabolic disorders, including obesity, dyslipidemia and metabolic dysfunction-associated steatohepatitis.

Sobetirome (GMP) is Sobetirome (HY-14823) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC₅₀ of 0.16 μM.

THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72).

KB-141 is a potent and selective TRβ agonist. The IC₅₀ values are 23.9 nM and 3.3 nM for binding affinities from displacement of T3 from hTRα1 and hTRβ1, respectively. KB-141 has anti-obesity, anti-diabetic, and lipid-lowering effects?and can be used as an anti-cholesteremic agent in vivo.

LL-340001 is the receptor-active metabolite released after hydrolysis of Elunetirom (HY-160207) by FAAH in the central nervous system. LL-340001 acts as a thyroid hormone receptor (TR) agonist, with potent full agonist activity at both TRα and TRβ. LL-340001 exhibits neuronal plasticity activity and can activate programs related to neuroplasticity and mitochondrial biogenesis in neuronal systems. LL-340001 can be used in the research of major depressive disorder and bipolar depression.

Trh-gly (TRH-glycine) is a precursor of thyrotropin (TSH)-releasing hormone (TRH) that can release thyrotropin and prolactin.

Kylo-0603 is an orally active thyroid hormone receptor β (THR-β) agonist with an EC₅₀ of 31.07 nM against human targets, and it exhibits much higher selectivity for THR-β than for THR-α. Kylo-0603 enables hepatocyte-targeted delivery via GalNAc modification. Kylo-0603 reduces serum cholesterol and low-density lipoprotein cholesterol levels. Kylo-0603 alleviates hepatic steatosis, inflammatory responses, hepatocyte ballooning, and non-alcoholic steatohepatitis activity scores. Kylo-0603 inhibits the progression of hepatic fibrosis. Kylo-0603 can be used for research on metabolic dysfunction-associated steatohepatitis (MASH).