MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases.

Cholic acid-Glu is a derivative of Cholic acid. The abundance of Cholic acid-Glu is increased in Crohn’s disease. Cholic acid-Glu increases PXR activation and significantly increases the expression of the downstream PXR target gene Cyp3a11 in small intestinal organoid tissue.

SJPYT-318 is a highly selective pregnane X receptor (PXR) agonist, targets PXR ligand-binding domain (LBD), exhibits selectivity for PXR LBD over LXR LBDs for recruiting SRC-1.

FKK6 (Felix Kopp Kortagere 6) is a specific human pregnane X receptor (hPXR) agonist with IC50 of 1.56 uM in a cell-free competitive hPXR TR-FRET-binding assays.

SR-12813 is a pregnane X receptor (PXR) agonist.

C2BA-4(C2BA 4) is a potent, specific human Pregnane X receptor (hPXR) activator with EC50 of 49 nM.