Chemical Name: (±)-(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline
Biological ActivityAntagonist 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). Structural 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
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VersaClone cDNA Plasmids
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