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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Pregnane X Receptor (PXR)-SPA70
SPA70

Chemical Structure : SPA70

CAS No.: 931314-31-7

SPA70 (PXR antagonist SPA70)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.
SPA70 displays highly selectivity over 10 other nuclear receptors (FXR, LXR, RXR, PPAR, etc.).
SPA70 antagonizes hPXR target genes induced by various hPXR agonists, blocks hPXR-mediated drug metabolism in vivo.

物理化学性质&存储条件

分子量 415.508
分子式 C21H25N3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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

参考文献

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

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