G-15
目录号 : GC16618
An antagonist of the estrogen receptor GPER
Cas No.:1161002-05-6
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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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].
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.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.701 mL | 13.5048 mL | 27.0095 mL |
| 5 mM | 0.5402 mL | 2.701 mL | 5.4019 mL |
| 10 mM | 0.2701 mL | 1.3505 mL | 2.701 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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