Sobetirome

Sobetirome

Catalog Number:
L002368880APE
Mfr. No.:
APE-A3828
Price:
$282
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      • Overview
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          Background

          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 clinical trials, Sobetirome was shown to be generally well tolerated at all doses studied and proof of the therapeutic concept of cholesterol lowering was clearly demonstrated 1.

          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.

      • Properties
        • Categories
          Agonist of tyroid hormone receptor
          Alternative Name
          GC-1; QRX-431; 2-[4-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-3,5-dimethylphenoxy]acetic acid
          CAS Number
          211110-63-3
          Molecular Formula
          C20H24O4
          Molecular Weight
          328.4
          Appearance
          White solid
          Purity
          98.00%
          Solubility
          ≥32.8 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥47.6 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C
          SMILES
          CC1=CC(=CC(=C1CC2=CC(=C(C=C2)O)C(C)C)C)OCC(=O)O

          * For Research Use Only

      • Reference
        • 1. McMillan, Jacob E., et al. "Multi-Generational Pharmacophore Modeling for Ligands to the Cholane Steroid-Recognition Site in the β1 Modulatory Subunit of the BKCa Channel." Journal of Molecular Graphics and Modelling (2014).

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