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Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist. PK properties of the TRβ agonist were analyzed by Medicilon.

2023-07-17

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Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.

Reference:

Qiu Li, et al. Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. J Med Chem. 2022 May 26;65(10):7193-7211. doi: 10.1021/acs.jmedchem.2c00144.

dyslipidemia NASH lipid-metabolism safety metabolic-stability pharmacokinetic-properties

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