SPA70 是一种有效的选择性人孕烷 X 受体 (hPXR) 拮抗剂，IC50 为 540 nM (Ki=390 nM)。 SPA70可以增强癌细胞的化学敏感性。
货号:ajcx25524
CAS:931314-31-7
分子式:C21H25N3O4S
分子量：415.5
溶解度:Chloroform: 10 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SPA70 is a pregnane X receptor (PXR) antagonist (IC₅₀= 0.51 µM).¹It 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 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 in human PXR transgenic (hPXR-tg) mice.

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