16α-LE2

16α-LE2 is a synthetic, steroidal estrogen and a highly potent, selective agonist of the estrogen receptor alpha (ERα), with 265-fold higher transactivation potency and 70–1000-fold higher binding affinity for ERα compared to ERβ. It mimics the estradiol core structure and is utilized in research to dissect the biological roles of ERα versus ERβ. 16α-LE2 shows strong selectivity for ERα in both human and animal models, stimulating uterine growth and protecting bone formation through ERα activation, while lacking effects on ovarian follicle development (an ERβ-mediated process). It was originally synthesized and patented by Schering AG.

Other names

16α-lactone-estradiol3,17β-dihydroxy-19-nor-17α-pregna-1,3,5(10)-triene-21,16α-lactone19-norpregna-1,3,5(10)-trien-21-oic acid, 3,16,17-trihydroxy-, gamma-lactone, (16α,17α)-