SR-12813 is a 1,1-bisphosphonate ester that exhibits hypocholesterolemic activity by enhancing the degradation of HMG-CoA reductase in various animal models. SR-12813 is also a high affinity ligand for human and rabbit pregnane X receptors (Kd = 41 nM; EC50 = 137 nM for hPXR in vitro) and can induce cytochrome P450 3A expression in human and rabbit hepatocytes.
