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SR 12813 is a PXR (pregnane X receptor) agonist (EC50 values are 200 and 700 nM for human and rabbit PXR respectively). SR 12813 activates the FXR (farnesoid X receptor) at μM concentrations. SR 12813 is an inhibitor of HMGCR.
Berkhout et al (1996) The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J.Biol.Chem. 271 14376. Jones et al (2000) The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. Mol.Pharmacol. 14 27. Lemaire et al (2007) Discovery of a highly active ligand of human pregnane X receptor: a case study from pharmacophore modeling and virtual screening to "in vivo" biological activity. Mol.Pharmacol. 72 572.
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