Description: G15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM). Target: Estrogen Receptor/ERR. Smiles: Brc1cc2OCOc2cc1[C@@H]1Nc2ccccc2[C@@H]2C=CC[C@H]12. References: Nayak T K , Bologa C G , Leitao A , et al. In vivo effects of a GPR30 antagonist[J]. Nature Chemical Biology, 2009, 5(6):421-427.

G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-15 is a cell-permeable...