gpr30

G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

GPR30 agonist-1 is a compound that acts as an agonist for G protein-coupled receptor 30 (GPR30), inducing vasorelaxation.

Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist (IC50=9.4 nM) and an agonist of GPR30. Fulvestrant has antitumor activity, inhibiting cell proliferation and inducing apoptosis and autophagy.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

Tectoridin (Shekanin) possesses an estrogenic and thyroid hormone-like agent by activating estrogen and thyroid hormone receptors. Tectoridin has anti-oxidant, anti-inflammatory and hypoglycemic activities; Tectoridin and its five metabolites inhibits the activities of lens aldose reductase in rat (IC : 1.4-15.5 μM).

G15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM)

Fulvestrant-d3 is a isotope labeled compound of Fulvestrant.Fulvestrant (ZM 182780) is an estrogen receptor (ER) antagonist and GPR30 agonist that inhibits cell proliferation and induces apoptosis and autophagy.