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SPA70

Chemical Structure : SPA70

CAS No.: 931314-31-7

SPA70 (SPA 70)

Catalog No.: PC-62523Not For Human Use, Lab Use Only.

SPA70 is a potent and selective hPXR antagonist (IC50=0.51 uM) that interacts with the ligand-binding domain (LBD) of hPXR, inhibits hPXR in human hepatocytes and mouse models and enhances the chemosensitivity of cancer cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SPA70 is a potent and selective hPXR antagonist (IC50=0.51 uM) that interacts with the ligand-binding domain (LBD) of hPXR, inhibits hPXR in human hepatocytes and mouse models and enhances the chemosensitivity of cancer cells; displays highly selectivity over 10 other nuclear receptors (FXR, LXR, RXR, PPAR, etc.); antagonizes hPXR target genes induced by various hPXR agonists, blocks hPXR-mediated drug metabolism in vivo.

Physicochemical Properties

M.Wt 415.508
Formula C21H25N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((4-(tert-butyl)phenyl)sulfonyl)-1-(2,5-dimethoxyphenyl)-5-methyl-1H-1,2,3-triazole

References

1. Lin W, et al. Nat Commun. 2017 Sep 29;8(1):741.

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