Formulation: A solid
Formal Name: 1-(2,5-dimethoxyphenyl)-4-[[4-(1,1-dimethylethyl)phenyl]sulfonyl]-5-methyl-1H-1,2,3-triazole
Purity: ≥90%
Formula Markup: C21H25N3O4S
Formula Weight: 415,5
Shelf life (days): 1460
CAS Number: 931314-31-7
Notes: SPA70 is a pregnane X receptor (PXR) antagonist (IC50 = 0.51 µM).{61652} It is selective for PXR over 10 additional nuclear receptors at concentrations greater than 5 µM, as well as over a panel of 384 kinases at 10 µM. SPA70 (0.1-10 µM) inhibits PXR activation induced by rifampicin (Item No. 14423) in HEK293 cells expressing the human receptor. It also inhibits rifampicin-induced activity of the PXR target cytochrome P450 (CYP) isoform 3A4 (CYP3A4) in primary human hepatocytes. SPA70 (200 mg/kg) inhibits PXR agonist-induced CYP3A4-mediated metabolism of midazolam and paclitaxel (Item No. 10461) in human PXR transgenic (hPXR-tg) mice.