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G-15

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Catalog No.
B5469
GPER受体拮抗剂
组合的产品项目
规格价格库存 数量
10mg
¥ 1,920.00
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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].

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.

文献引用

1.Zhong J, Ge HF, et al. "G Protein-Coupled Estrogen Receptor 1 Negatively Regulates the Proliferation of Mouse-Derived Neural Stem/Progenitor Cells via Extracellular Signal-regulated Kinase Pathway." Brain Res. 2019 Feb 21. pii:S0006-8993(19)30108-8. PMID:30797747
2.Chang Y, Han Z, et al. "G protein-coupled estrogen receptor activation improves contractile and diastolic functions in rat renal interlobular artery to protect against renal ischemia reperfusion injury." Biomed Pharmacother. 2019 Apr;112:108666. PMID:30784936
3.Wu Y, Feng D, et al. "Downregulation of G protein coupled receptor 30 in the hippocampus attenuates the neuroprotection of estrogen in the critical period hypothesis." Mol Med Rep. 2018 Apr;17(4):5716-5725. PMID:29484405

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt370.24
Cas No.1161002-05-6
FormulaC19H16BrNO2
Solubility≥37mg/mL in DMSO
Chemical Name(3aR,4S,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
SDFDownload SDF
Canonical SMILESBrC1=C([C@H]2NC3=CC=CC=C3[C@]4([H])[C@@]2([H])CC=C4)C=C5OCOC5=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1,2]:

细胞系

永生化上皮内膜异位细胞系(11z)

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10、30或60 μM,24、48或72小时

应用

G-1(30 μM)在2小时内导致Akt的serine 473位磷酸化。用G-15(60 μM)预处理可防止G-1诱导的磷酸化。10 μM G-1处理72小时显著刺激细胞增殖,随后用30 μM G-15处理72小时显著逆转了这种刺激。G-15减少相对增殖。G-15以剂量依赖性方式抑制SKBr3细胞中G-1介导的钙动员,IC50大约为185 nM。在GPR30转染的COS7细胞中,G-15抑制G-1介导的PI(3)K的激活。

Animal experiment [3]:

动物模型

卵巢切除的雌性大鼠

给药剂量

皮下注射,5 μg/day,10 μg/day

应用

G-15以剂量依赖性方式损害DMP获取。G-15特异性减少获取速率。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Imesch P, Samartzis E P, Dedes K J, et al. Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells[J]. Fertility and sterility, 2013, 100(3): 770-776.

[2]. Dennis M K, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist[J]. Nature chemical biology, 2009, 5(6): 421-427.

[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[J]. Hormones and behavior, 2012, 62(4): 367-374.

质量控制

质量控制和MSDS

批次:

化学结构

G-15

相关生物数据

G-15

相关生物数据

G-15

相关生物数据

G-15