| 货号 | 14397-1mg |
| 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-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol (Item No. 10006315) or the GPER-selective agonist G-1 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).3 It has no detectable binding activity to either ERα or ERβ.3 G-36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF.3 G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.3,4 |
| 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.,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). 4.Brailoiu, G.C.,Arterburn, J.B.,Oprea, T.I., et al. Bradycardic effects mediated by activation of G protein-coupled estrogen receptor in rat nucleus ambiguus. Experimental Physiology 98(3), 679-691 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 412.3 |
| 分子式 | C22H22BrNO2 |
| CAS号 | 1392487-51-2 |
| 稳定性 | ≥ 2 years |
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