Antagonist of GPER; selectively inhibits estrogen-mediated activation of PI3-K by GPER, but not by ERα
. Also inhibits estrogen-mediated calcium mobilization (IC50
= 112 nM). Analog of G-1
(Cat. No. 3577).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
The G-protein-coupled estrogen receptor GPER in health and disease.
Prossnitz and Barton
Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity.
Dennis et al.
J.Steroid Biochem.Mol.Biol., 2011;127:358