Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%)
靶点:
ERα
体外研究:
The EC50 of Propyl pyrazole triol for the ERα-dependent response is 140 pM in ERα-U2OS-Luc cells.
参考文献:
1. Influence of cellular ERalpha/ERbeta ratio on the ERalpha-agonist induced proliferation of human T47D breast cancer cells. 2. Stauffer SR, et al. Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-alpha-selective agonists. J Med Chem. 2000 Dec 28;43(26):4934-47