G36

G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC₅₀=112 nM). G-36 is promising for research in the field of cancer^[1][2]. In Vitro:G36 (1 µM, 15 minutes) demonstrates inhibitory activity on GPER-mediated ERK activation, effectively blocking E2- and G-1 (HY-107216)-induced ERK activation in SKBr3 cells^[1].
G36 (10 µM, 30 minutes) inhibits endothelin-1- and G-1 (HY-107216)-induced contraction of porcine coronary artery rings, indicating its ability to effectively block GPER-mediated coronary artery tension regulation^[2].
In Vivo:G36 (50 µg/kg, s.c., single dose) demonstrates significant GPER antagonistic activity in the ovariectomy-induced estrogen-dependent uterine hyperplasia C57Bl6 mouse model, effectively inhibiting E2-induced uterine epithelial cell proliferation^[1].