| 货号 | 14673-1mg |
| 描述 | G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.1 It is thought to be involved in estrogen-sensitive cancers.1,2 GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.1 G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).3 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.4 G-15 antagonizes the anti-depressive effects of estrogen in vivo.3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Filardo, E.J. and Thomas, P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 153(7), 2953-2962 (2012). 2.Chevalier, N.,Vega, A.,Bouskine, A., et al. GPR30, the non-classical membrane G protein related estrogen receptor, is overexpressed in human seminoma and promotes seminoma cell proliferation. PLoS One 7(4), 34672 (2012). 3.Dennis, M.K.,Burai, R.,Ramesh, C., et al. In vivo effects of a GPR30 antagonist. Nature Chemical Biology 5(6), 421-427 (2009). 4.Dennis, M.K.,Field, A.S.,Burai, R., et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. Journal of Steroid Biochemistry and Molecular Biology 127(3-5), 358-366 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 370.2 |
| 分子式 | C19H16BrNO2 |
| CAS号 | 1161002-05-6 |
| 稳定性 | ≥ 2 years |
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