Uses
SR 12813 is a pregnane X receptor (PXR, NR 112) agonist.
Definition
ChEBI: An organic phosphonate that is the tetraethyl ester of [2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethene-1,1-diyl]bis(phosphonic acid).
Biological Activity
Pregnane X receptor (PXR) agonist (EC 50 values are 200 and 700 nM for human and rabbit PXR respectively). Activates the farnesoid X receptor (FXR) at μ M concentrations. Displays hypocholesterolaemic activity via enchanced degradation of HMG-CoA reductase.
Biochem/physiol Actions
SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity. It decreases the biosynthesis of cholesterol by enhancing the degradation of HMG-CoA reductase.
