Catalog No.: PC-24990Not For Human Use, Lab Use Only.
MI891 is a potent, selective pregnane X receptor (PXR) inverse agonist/antagonist, displays antagonistic activity with an IC50 of 378 nM for rifampicin (1 μM)-activated PXR, binds to the ligand-binding domain (LBD) of PXR.
MI891 is a potent, selective pregnane X receptor (PXR) inverse agonist/antagonist, displays antagonistic activity with an IC50 of 378 nM for rifampicin (1 μM)-activated PXR, binds to the ligand-binding domain (LBD) of PXR.
MI891 exhibits inverse agonistic activity with an IC50 of 6.1 μM and maximal inhibition of 68.8 ± 5.5% at 10 μM.
MI891 also suppresses both rifampicin-induced and basal (constitutive) CYP3A4 mRNA expression in HepaRG cells in a concentration-dependent manner.
MI891 binding (MST, KD=1.7 uM) abrogates PXR LBD coactivation with steroid receptor coactivator 1 (SRC1).
MI891 shows no binding activity on CAR, and no significant agonistic or antagonistic activities of MI891 on human VDR, FXR, LXRβ, LXRα, and PPARα receptors.
