SPA70 is a potent and selective human pregnane X receptor (hPXR) antagonist with IC50 values of 510 nM (cell-based hPXR antagonistic assay) and 540 nM (cell-free competitive hPXR TR-FRET-binding assay). SPA70 inhibits hPXR in human hepatocytes and humanized mouse models and enhances the chemosensitivity of cancer cells, consistent with the role of hPXR in drug resistance.

KEYWORDS: SPA70 | supplier | hPXR antagonist | LC-1 | Specific PXR antagonist 70 | SPA 70 | SPA-70 | LC 1 | LC1 | CAS [931314-31-7] | Metabolism | PXR | Antagonist | Receptors | Cancer | Hepatocyte