Chemical Name:4,4',4''-(4-Propyl-[1H]-pyrazole-1,3,5-triyl)trisphenol
Biological Activity:
Potent,
subtype-selective estrogen receptor agonist (EC50 ~ 200 pM);
displays 410-fold selectivity for ERα over ERβ. Prevents ovariectomy-induced weight
gain and loss of bone mineral density, and induces gene expression in the
hypothalamus following systemic administration in vivo.
Staufferet al (2000) Pyrazole
ligands: structure-affinity/activity relationships and estrogen
receptor-alpha-selective agonists. J.Med.Chem. 43 4934. Kraichelyet al (2000) Conformational changes and coactivator recruitment by novel
ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations
with biological character and distinct differences among SRC coactivator family
members. Endocrinology 141 3534. Harriset al
(2002) Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in
vivo through the use of an ERα-selective ligand. Endocrinology 143
4172.
