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Sobetirome

Catalog No. T5313 CAS 211110-63-3

Synonyms: IACS-010759, QRX-431

Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).

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Sobetirome, CAS 211110-63-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 59.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 147.00
25 mg	In stock	$ 297.00
50 mg	In stock	$ 593.00
100 mg	In stock	$ 842.00
200 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 98.72%

Purity: 98.25%

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Description	Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).
Targets&IC50	TRα 1:0.58 μM (EC50), TRβ 1:0.16 μM (EC50)
In vitro	GC-1 was designed to bind selectively to TRβ (EC50: 0.58 μM for TRα-1, 0.16 μM for TRβ-1) [1]. The thyromimetic agent GC-1 induces hepatocyte proliferation via Wnt/β-catenin signaling and may promote regeneration in both acute and chronic liver insufficiencies [2].
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	IACS-010759, QRX-431
Molecular Weight	328.4
Formula	C20H24O4
CAS No.	211110-63-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (91.4 mM)

Ethanol: 30 mg/mL

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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Clinical Compound Library Bioactive Compound Library NO PAINS Compound Library Human Metabolite Library Bioactive Compounds Library Max Pediatric Drug Library Nuclear Receptor Compound Library Endocrinology-Hormone Compound Library ReFRAME Related Library

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Keywords

Sobetirome 211110-63-3 Endocrinology/Hormones Thyroid hormone receptor(THR) QRX431 Inhibitor IACS010759 IACS-010759 GC1 inhibit QRX-431 IACS 010759 Thyroid Hormone Receptor QRX 431 GC-1 GC 1 THR inhibitor

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