Drug intelligence / Profile preview

SR12813

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

SR12813 is a synthetic small molecule that acts as an agonist of the pregnane X receptor (PXR), with EC50 values of approximately 200 nM for human PXR. It also activates the farnesoid X receptor (FXR) at micromolar concentrations. SR12813 displays hypocholesterolemic activity by promoting enhanced degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase), thereby inhibiting cholesterol synthesis in vitro and in vivo. The compound has been shown to increase LDL receptor expression and LDL uptake in hepatocytes. It is primarily used as a research tool to study nuclear receptor biology and cholesterol metabolism[1][3][7][8].

Other names
tetraethyl (2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethene-1,1-diyl)bis(phosphonate)tetraethyl [2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethene-1,1-diyl]bis(phosphonate)4-[2,2-bis(diethoxyphosphoryl)ethenyl]-2,6-di-tert-butylphenol
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)FXR (Farnesoid x-activated receptor)PXR (Pregnane X receptor)

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