| Bioactivity | 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[1]. | ||||||||||||
| Target | EC50: 0.16 μM (TRβ-1), 0.58 μM (TRα-1) | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | Sobetirome | ||||||||||||
| CAS | 211110-63-3 | ||||||||||||
| Formula | C20H24O4 | ||||||||||||
| Molar Mass | 328.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |