SPA70

SPA70

CAT N°: 34490
Price:

From 48.00 40.80

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.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 1-(2,5-dimethoxyphenyl)-4-[[4-(1,1-dimethylethyl)phenyl]sulfonyl]-5-methyl-1H-1,2,3-triazole
  • Correlated keywords
    • SPA-70 LC1 LC-1 HEK-293 P-450 CYP-3A4 CYP3-A4
  • Product Overview:
    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.

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