THR-β agonist 9 

THR-β agonist 9 is a potent, selective, and His435 mutation-sensitive THR-β (EC₅₀: 3.2 nM) agonist. THR-β agonist 9 has moderate selectivity (approximately 10-fold) and good activation capacity (EC₅₀: 134.2 nM to 515.5 nM) for multiple His435 mutants (H435A, H435Y, and H435R). THR-β agonist 9 has the potential to be used in the study of dyslipidemia, metabolic dysfunction-associated steatohepatitis (MASH), or resistance to thyroid hormone (RTH)^[1].

THR-β with an EC50 of 258.2 nM

THR-β agonist 9 (Compound 15n) (1 μM) can activate THR-β with an EC₅₀ of 258.2 nM and a potency of 1707.0 nM for THR-α, showing excellent selectivity in cell-based reporter gene assays^[1].

THR-β agonist 9 simultaneously activates three mutants with EC₅₀s of THR-β^H435A (515.5 nM), THR-β^H435R (134.2 nM) and THR-β^H435Y (513.1 nM)^[1].

THR-β agonist 9 (1-10 μM, 24 hours) can reduce TG and TC levels and lipid accumulation in mouse primary hepatocytes and HepG2 cells^[1].

THR-β agonist 9 (1-10 μM, 24 hours) increases basal and uncoupled mitochondrial respiration in HepG2 cells^[1].

THR-β agonist 9 (1-10 μM, 24 hours) increases the phosphorylation of AMPK and ACC, accompanied by higher CPT1 protein levels, improving the metabolism of HepG2 cells through the AMPK pathway^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

418.40

C₂₃H₁₈N₂O₆

2920045-74-3

OC1=C(C(NCC(O)=O)=O)N=C(OC)C2=CC(OC3=CC=C4C(C=CC=C4)=C3)=CC=C21

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Li Q, et al. Discovery of a Potent, Selective, and Multiple His435 Mutation-Sensitive Thyroid Hormone Receptor β Agonist. J Med Chem. 2025 Jul 10;68(13):13471-13490.  [Content Brief]