产品描述:
G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.{23445} It is thought to be involved in estrogen-sensitive cancers.{23445,23446} GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.{23445} G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol (Item No. 10006315) or the GPER-selective agonist G-1 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).{23443} It has no detectable binding activity to either ERα or ERβ.{23443} G-36 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.{23443} 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.{23443,24423}