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G-15
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
G-15图片
CAS NO:1161002-05-6
规格:98%
分子量:370.24
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
GPER receptor antagonist
CAS:1161002-05-6
分子式:C19H16BrNO2
分子量:370.24
纯度:98%
存储:Store at -20°C

Background:

G-15 is a selective antagonist of GPR30 with Ki value of 20 nM [1].


G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].


G-15 is a selective GPR30 antagonist with Ki value of 20 nM, While displayed little binding to ERα or ERβ up to 10 μM. In SKBr3 breast cancer cells that expressed only GPR30, G-1 or estrogen significantly increased intracellular calcium concentrations, while G15 inhibited the response to G-1 or estrogen with IC50 value of 185 and 190 nM respectively in a dose-dependent way. In GPR30-transfected COS7 cells, G-15 inhibited both estrogen and G-1 activation of PI3K and accumulation of PIP3 [1]. In endometriotic cells, G-1 increased cell proliferation and Akt phosphorylation, while G-15 reversed this stimulation and inhibited cell proliferation and induced Akt dephosphorylation [2].


In intact rats and ovariectomized (OVX) rats treated with estradiol, G-15 impaired acquisition of delayed matching-to-position (DMP) T-maze task with a persistent turn. The result suggested that GPR30 played an crucial role in mediating the effects of estradiol on spatial learning [3].


参考文献:
[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.