Sobetirome GC-1

Sobetirome GC-1

Sobetirome GC-1 is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM.[1]

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Sobetirome is a thyroid hormone receptor isoform beta-1 liver-selective analog with antilipidemic and antiatherosclerotic activity. In animal models sobetirome reduced serum lipids, decreased cholesterol levels, and stimulated steps of reverse cholesterol transport, which promotes the reverse transport of cholesterol from atherogenic macrophages back to the liver for excretion. In humans, sobetirome lowered plasma LDL cholesterol and reduced plasma triglycerides, while its liver-selective activity helped avoid the side effects seen with many other thyromimetic agents.

Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)- and liver uptake-selective agonist. Sobetirome (48 nmol/kg) reduces high-density lipoprotein (HDL) cholesterol and very low-density lipoprotein (VLDL) triglyceride levels in euthyroid Mice. Sobetirome reduces HDL cholesterol and triglyceride Levels in hypercholesterolemic mice. Sobetirome increases hepatic HDL receptors and stimulates bile acid synthesis in hypercholesterolemic mice[2]. Treatment with 10× Sobetirome (GC-1) results in a gain of fat mass of only 21% (1.7 g), and treatment with 20× Sobetirome (GC-1) induces a decrease in fat mass of 20% (1.3 g)[3].

This research sample contains 3000 mcg of Sobetirome GC-1 suspended in 30 mL of PEG 400.

Compound Description

[1]. Gierach I, et al. Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors α-1 and β-1. FEBS Open Bio. 2012 Aug 15;2:247-53.

[2]. Johansson L, 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 U S A. 2005 Jul 19;102(29):10297-302.

[3]. Villicev CM, et al. Thyroid hormone receptor beta-specific agonist GC-1 increases energy expenditure and prevents fat-mass accumulation in rats. J Endocrinol. 2007 Apr;193(1):21-9.