GC 1

Biological Activity

GC 1 is a thyromimetic; high affinity agonist at thyroid hormone receptor (TR) β and TRα receptors (K_D values are 67 and 440 pM respectively). Displays 5- and 100-fold greater potency than the endogenous agonist T₃ in vitro at TRα₁ and TRβ₁ receptors respectively. Promotes reverse cholesterol transport in chow- and fat-fed mice. Induces proliferation of hepatocytes and pancreatic acinar cells in rats independent of prior tissue injury.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Selective thyroid receptor modulation by GC-1 reduces serum lipids stimulates steps of reverse cholesterol transport in euthyroid mice.
   Johansson, L et al.
   PNAS 102(29): 10297-10302.
2. An Activating STAT3 Mutation Causes Neonatal Diabetes through Premature Induction of Pancreatic Differentiation
   J Saarimäki-, D Balboa, MA Russell, J Saarikettu, M Kinnunen, S Keskitalo, A Malhi, C Valensisi, C Andrus, S Eurola, H Grym, J Ustinov, K Wartiovaar, RD Hawkins, O Silvennoin, M Varjosalo, NG Morgan, T Otonkoski
   Cell Rep, 2017;19(2):281-294.
3. A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
   Chiellini et al.
   Chem.Biol., 1998;5:299
4. The thyroid hormone receptor-β agonist GC-1 induces cell proliferation in rat liver and pancreas.
   Columbano et al.
   Endocrinology, 2006;147:3211

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