QRX 431

The Uses of QRX 431

GC 1 is a high affinity thyroid receptor α (TRα) and TRβ agonist.

Definition

ChEBI: Sobetirome is a diarylmethane.

Biological Activity

sobetirome (3,5-dimethyl-4[(4'-hydroxy-3'-isopropylbenzyl)-phenoxy] acetic acid, also known as gc-1 and qrx-431, is a member of a class of compounds known as selective thyromimetics.it was firstly developed by thomas scanlan’s group at the university of california-san francisco (ucsf) in 1995 1.in cholesterol-fed rats, sobetirome was shown to lower plasma cholesterol in a dose-dependent manner by up to 75% of untreated controls. in hypercholesterolemic mice, sobetirome was failed to induce ldl receptor mrna expression. in different mouse models, sobetirome and t-0681 were shown to promote bile acid production and biliary sterol secretion. in cynomolgus monkeys, sobetirome was shown to reduce plasma cholesterol in a dose-dependent manner by up to 30%. both sobetirome and t-0681 were shown to increase hepatic expression of the hdl receptor (scavenger receptor-bi, sr-bi) in animals.in phase i

Biochem/physiol Actions

Sobetirome is also termed as 2-(4-(4-(benzyloxy)-3-isopropylbenzyl)-3,5-dimethylphenoxy)acetic acid/ GC-1. It has an inner-ring and negatively charged carboxylate groups at physiological pH. Sobetirome is considered as a cholesterol lowering agent in humans.

Storage

Store at -20°C

References

1. tancevski i, demetz e, eller p. sobetirome: a selective thyromimetic for the treatment of dyslipidemia. recent pat cardiovasc drug discov. 2011 jan;6(1):16-9.