"目录号: HY-14823
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。
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
Thomas S. Scanlan-Oregon Health and Science University
X-Linked Adrenoleukodystrophy-Adrenomyeloneuropathy
April 2013
Phase 1
NeuroVia, Inc.
X-linked Adrenoleukodystrophy
October 1, 2017
Phase 1-Phase 2
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References
