propylpyrazoletriol

Propylpyrazoletriol (PPT) is a synthetic, nonsteroidal selective agonist of estrogen receptor alpha (ERα) with approximately 410-fold selectivity for ERα over estrogen receptor beta (ERβ). It exhibits a relative binding affinity of 49% for ERα compared to 0.12% for ERβ, with an EC50 of approximately 140-200 pM for ERα-dependent responses. PPT is widely used in scientific research to study the function of ERα. Though originally thought to be highly selective for ERα, it has subsequently been found to also act as an agonist of the G protein-coupled estrogen receptor (GPER/GPR30). In preclinical studies, PPT prevents ovariectomy-induced weight gain and loss of bone mineral density, and induces gene expression in the hypothalamus following systemic administration. It has also demonstrated anti-diabetic effects in mouse models and effects on male sexual function in rat models.

Other names

propyl pyrazole triol1,3,5-tris(4-hydroxyphenyl)-4-propyl-1H-pyrazole4,4',4''-(4-propyl-1H-pyrazole-1,3,5-triyl)triphenol4,4',4''-(4-propylpyrazole-1,3,5-triyl)trisphenol