A PXR antagonist
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SPA70

Item No. 34490

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2,5-dimethoxyphenyl)-4-[[4-(1,1-dimethylethyl)phenyl]sulfonyl]-5-methyl-1H-1,2,3-triazole
CAS Number
931314-31-7
Synonyms
  • Specific PXR Antagonist 70
Molecular Formula
C21H25N3O4S
Formula Weight
415.5
Purity
≥90%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: 10 mg/ml
λmax
234 nm
SMILES
COC1=CC(N2N=NC(S(C3=CC=C(C(C)(C)C)C=C3)(=O)=O)=C2C)=C(OC)C=C1
InChi Code
InChI=1S/C21H25N3O4S/c1-14-20(29(25,26)17-10-7-15(8-11-17)21(2,3)4)22-23-24(14)18-13-16(27-5)9-12-19(18)28-6/h7-13H,1-6H3
InChi Key
OIOPHIFJQXHPAF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    25 mg

    $587

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    Product Description

    SPA70 is a pregnane X receptor (PXR) antagonist (IC50 = 0.51 µM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lin, W., Wang, Y.-M., Chai, S.C., et al. SPA70 is a potent antagonist of human pregnane X receptor. Nat. Commun. 8(1), 741 (2017).