Description
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 (Ki = 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.
Uses
(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.
in vivo
G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice[1].
| Animal Model: | Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1] |
| Dosage: | 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) |
| Administration: | Subcutaneous injection; twice a week for 14 weeks |
| Result: | The number of tumor nodules decreased in the E2+Ful+G15 group. |
storage
-20°C, protect from light
References
[1] dennis mk, burai r, ramesh c, et al. in vivo effects of a gpr30 antagonist. nat chem biol, 2009, 5 (6): 421-427.
[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.
