"目录号: HY-14823

Metabolic Enzyme/Protease-

Sobetirome 是一种甲状腺激素受体 β (TRβ)激动剂，Sobetirome 选择性结合到TRβ-1，EC50为 0.16 μM。

LXR

相关产品

GW3965 hydrochloride-LXR-623-SR9243-T0901317-AZ876-27-Hydroxycholesterol-BMS-779788-24-Hydroxycholesterol-BMS-852927-

生物活性

Description

Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively toTRβ-1withEC50of 0.16 μM.

IC50& Target

EC50: 0.16 μM (TRβ-1), 0.58 μM (TRα-1)[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].

Clinical Trial

NCT01787578

Thomas S. Scanlan-Oregon Health and Science University

X-Linked Adrenoleukodystrophy-Adrenomyeloneuropathy

April 2013

Phase 1

NCT03196765

NeuroVia, Inc.

X-linked Adrenoleukodystrophy

October 1, 2017

Phase 1-Phase 2

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References

[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.