(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline

G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-15 is a cell-permeable non-steroidal antagonist of GPER (K_i = 20 nM). It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ERα, so that at doses greater than 1 μM it is capable of mediating limited ER-dependent transcriptional activity. G-15 antagonizes the anti-depressive effects of estrogen in vivo.

(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline is also known as “G-15”, a G-protein-coupled estrogen receptor antagonist designed for the treatment of estrogen-sensitive cancers.

Store at -20°C

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[2] g-protein-coupled estrogen receptor and the gper-antagonist g-15 inhibits proliferation in endometriotic cells. fertil steril, 2013, 100 (3): 770-776.
[3] hammond r, nelson d, kline e, et al. chronic treatment with a gpr30 antagonist impairs acquisition of a spatial learning task in young female rats. horm behav, 2012, 62 (4): 367-374.