An agonist of TRβ
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Sobetirome

Item No. 30814

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-[[4-hydroxy-3-(1-methylethyl)phenyl]methyl]-3,5-dimethylphenoxy]-acetic acid
CAS Number
211110-63-3
Synonyms
  • GC-1
  • QRX 431
Molecular Formula
C20H24O4
Formula Weight
328.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/mlEthanol: 30 mg/ml
SMILES
OC1=C(C(C)C)C=C(CC2=C(C)C=C(OCC(O)=O)C=C2C)C=C1
InChi Code
InChI=1S/C20H24O4/c1-12(2)17-9-15(5-6-19(17)21)10-18-13(3)7-16(8-14(18)4)24-11-20(22)23/h5-9,12,21H,10-11H2,1-4H3,(H,22,23)
InChi Key
QNAZTOHXCZPOSA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    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 Kd 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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).