Sobetirome

Sobetirome is an agonist of thyroid hormone receptor β (TRβ; EC₅₀ = 7 nM in a reporter assay).¹ It selectively binds to TRβ over TRα with K_d values of 0.1 and 1.8 nM, respectively. Sobetirome (97 nmol/kg, i.p.) increases hepatic levels of the HDL receptor SR-B1 and serum levels of C4, a marker of increased bile acid synthesis, in mice fed normal chow or high-cholesterol diets.² It reduces serum cholesterol and triglyceride levels in these same models. Sobetirome (154 nmol/kg, i.p.) also decreases plasma cholesterol levels, without increasing heart rate, in a mouse model of hypothyroidism induced by an iodine-deficient diet containing the thyroid hormone biosynthesis inhibitor 5-propyl-2-thio-uracil.³

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1. Nguyen, N.-H., Apriletti, J.W., Cunha Lima, S.T., et al. Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment. J. Med. Chem. 45(15), 3310-3320 (2002).

2. Johansson, L., Rudling, M., Scanlan, T.S., et al. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice. Proc. Natl. Acad. Sci. USA 102(29), 10297-10302 (2005).

3. Trost, S.U., Swanson, E., Gloss, B., et al. The thyroid hormone receptor-β-selective agonist GC-1 differentially affects plasma lipids and cardiac activity. Endocrinology 141(9), 3057-3064 (2000).