SPA70

Names

[ Name ]:
SPA70

[Synonym ]:
MFCD14774311
1H-1,2,3-Triazole, 1-(2,5-dimethoxyphenyl)-4-[[4-(1,1-dimethylethyl)phenyl]sulfonyl]-5-methyl-
1-(2,5-Dimethoxyphenyl)-5-methyl-4-{[4-(2-methyl-2-propanyl)phenyl]sulfonyl}-1H-1,2,3-triazole

Biological Activity

[Description]:

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.

[References]

References 1. Lin W, et al. Nat Commun. 2017 Sep 29;8(1):741. View Related Products by Target Pregnane X Receptor (PXR)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
612.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₂₅N₃O₄S

[ Molecular Weight ]:
415.506

[ Flash Point ]:
324.3±34.3 °C

[ Exact Mass ]:
415.156586

[ LogP ]:
4.01

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.586

Related Compounds

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