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Endocrinology/Hormones Thyroid hormone receptor(THR) Sobetirome

Sobetirome

Catalog No. T5313   CAS 211110-63-3
Synonyms: QRX-431, IACS-010759, QRX-431 IACS-010759

Sobetirome is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).

Sobetirome, CAS 211110-63-3
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1 mg In Stock 50.00
5 mg In Stock 110.00
10 mg In Stock 166.00
25 mg In Stock 362.00
50 mg In Stock 676.00
1 mL * 10 mM (in DMSO) In Stock 121.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sobetirome is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).
Targets&IC50 TRβ-1 :ic50 0.16 μM (EC50),   TRα-1 :ic50 0.58 μM (EC50),  
In vivo Four weeks following injection, mice were fed 5 mg/kg GC-1 or basal diet for 10 or 21 days. Treatment with GC-1 for 10 or 21 days led to a significant reduction in tumor burden [2]. GC-1 treatment reduced serum cholesterol levels by 25% and serum triglycerides by 75% in chow-fed mice and also attenuated diet-induced hypercholesterolemia [3]. GC-1 (50 or 100 mug/100 g body weight) strongly stimulates rat hepatocyte proliferation in the absence of tissue injury. GC-1 also induced massive pancreatic cell proliferation [4].
Animal Research
Briefly, 20 μg of a pT3-EF5α-hMet-V5 and pT3-EF5α-S45Y-β-catenin-Myc combination along with the transposase in a ratio of 25:1 were diluted in 2 mL of normal saline (0.9% NaCl), filtered through a 0.22-μm filter, and injected into the lateral tail vein of 23 FVB mice that were around 6 weeks old, in 5 to 7 seconds. These mice are referred henceforth as hMet-mutant-β-catenin mice. Four weeks after injection, hMet-mutant-β-catenin mice were randomized into two groups. One group was kept on a basal diet (n = 12), and another group was switched to a GC-1–supplemented diet (5 mg/kg of diet) (n = 11). Animals on control diet were sacrificed at either 21 days (n = 8) or 10 days (n = 4) after initiation of the diet. Similarly, animals on the GC-1 diet were sacrificed at either 21 days (n = 7) or 10 days (n = 4) after initiation of the diet. The animals were given access to food and water ad libitum with a 12-hour light/dark daily cycle. One intraperitoneal injection of bromodeoxyuridine (BrdU) was performed on day 9 during 10 days of GC-1 or basal diet treatment, and livers were harvested 24 hours later [2].
Synonyms QRX-431 , IACS-010759 , QRX-431 IACS-010759
Purity 98.25%
Molecular Weight 328.4
Formula C20H24O4
CAS No. 211110-63-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 30 mg/mL (91.4 mM)

Ethanol: 30 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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. Puliga E, et al. Thyroid Hormone Receptor-β Agonist GC-1 Inhibits Met-β-Catenin-Driven Hepatocellular Cancer. Am J Pathol. 2017 Nov;187(11):2473-2485. 3. 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. 4. Columbano A, et al. The thyroid hormone receptor-beta agonist GC-1 induces cell proliferation in rat liver and pancreas. Endocrinology. 2006 Jul;147(7):3211-8.

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