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SPA70
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SPA70图片
CAS NO:931314-31-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
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。
Cas No.931314-31-7
Canonical SMILESCOC1=CC(N2N=NC(S(C3=CC=C(C(C)(C)C)C=C3)(=O)=O)=C2C)=C(OC)C=C1
分子式C21H25N3O4S
分子量415.5
溶解度Chloroform: 10 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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)