G-15

Name: G-15
Brand: Tocris Bioscience
SKU: 3678
Rating: 3 (1 reviews)

Cat. No. 3678 31 篇引用文献 1 条评论提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： High affinity and selective GPER antagonist

化学名： (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline

纯度： ≥99% (HPLC)

说明书

引用文献 (31)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for G-15

G-15 is a high affinity and selective GPER receptor antagonist (K_i = 20 nM) that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC₅₀ of ~185 nM) and antagonizes the antidepressive and renoprotective effects of estrogen in vivo.

技术数据 for G-15

分子量	370.24
公式	C₁₉H₁₆BrNO₂
储存	Store at -20°C
纯度	≥99% (HPLC)
CAS Number	1161002-05-6
PubChem ID	90488870
InChI Key	LBBDCJLRQXMUAE-FWHYVADDSA-N
Smiles	BrC1=CC4=C(OCO4)C=[C@@]1[C@@H]2NC(C=CC=C5)=C5[C@@]3([H])[C@@]([H])2CC=C3.BrC6=CC9=C(OCO9)C=[C@@]6[C@H]7NC(C=CC=C%10)=C%10[C@]8([H])[C@]([H])7CC=C8

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for G-15

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	18.51	50

制备储备液 for G-15

以下数据基于产品分子量 370.24。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
0.5 mM	5.4 mL	27.01 mL	54.02 mL
2.5 mM	1.08 mL	5.4 mL	10.8 mL
5 mM	0.54 mL	2.7 mL	5.4 mL
25 mM	0.11 mL	0.54 mL	1.08 mL

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产品说明书 for G-15

分析证书/产品说明书

化学品安全技术说明书

参考文献 for G-15

参考文献是支持产品生物活性的出版物。

Dennis et al (2009) In vivo effects of a GPR30 antagonist. Nat.Chem.Biol. 5 421 PMID: 19430488

Hutchens et al (2012) Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo. Am.J.Physiol.Renal Physiol. 303 377 PMID: 22622457

Yue et al (2019) Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate. ACS Chem.Neurosci. 10 4227 PMID: 31545891

If you know of a relevant reference for G-15, please let us know.

按标靶查看相关产品

Estrogen (GPER) Receptors

关键词: G-15, G-15 supplier, high, affinity, selective, GPR30, antagonist, estrogen, oestrogen, receptors, GPER, Estrogen, (GPER), Receptors, 3678, Tocris Bioscience

31 篇 G-15 的引用文献

引用文献是使用了 Tocris 产品的出版物。 G-15 的部分引用包括：

Alicja et al (2022) Nuclear and Membrane Receptors for Sex Steroids Are Involved in the Regulation of Delta/Serrate/LAG-2 Proteins in Rodent Sertoli Cells. Int J Mol Sci 23 PMID: 35216398

Sandner et al (2014) Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility. Andrology 2 695 PMID: 25052196

S et al (2014) Activation of membrane estrogen receptors attenuates opioid receptor-like1 receptor-mediated antinociception via an ERK-dependent non-genomic mechanism. Neuroscience 255 177-90 PMID: 24452062

Manran et al (2013) GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer. Breast Cancer Res 15 R114 PMID: 24289103

Stephen D et al (2020) G Protein-Coupled Estrogen Receptor Regulates Actin Cytoskeleton Dynamics to Impair Cell Polarization. Front Cell Dev Biol 8 592628 PMID: 33195261

Mei-Ling et al (2020) G Protein-Coupled Estrogen Receptor Mediates Cell Proliferation through the cAMP/PKA/CREB Pathway in Murine Bone Marrow Mesenchymal Stem Cells. Int J Mol Sci 21 PMID: 32899453

David A et al (2020) GPER Activation Inhibits Cancer Cell Mechanotransduction and Basement Membrane Invasion via RhoA. Cancers (Basel) 12 PMID: 31991740

Francesco et al (2019) Low-dose Bisphenol-A regulates inflammatory cytokines through GPR30 in mammary adipose cells. J Mol Endocrinol 63 273-283 PMID: 31546233

Kanageswaran et al (2016) Modulatory Effects of Sex Steroids Progesterone and OE on Odorant Evoked Responses in Olfactory Receptor Neurons. PLoS One 11 e0159640 PMID: 27494699

Francesco et al (2014) GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res 74 4053 PMID: 24894716

Duncan et al (2012) 2-MethoxyOE inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A 109 21034 PMID: 23213242

Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -OE in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951

Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Mol Med Rep 6 894 PMID: 26441850

Chen et al (2015) G-protein-coupled receptor 30-mediated antiapoptotic effect of estrogen on spinal motor neurons following injury and its underlying mechanisms. Sci Rep 12 1733 PMID: 25872489

Villa et al (2015) Estrogen accelerates the resolution of inflammation in macrophagic cells. Breast Cancer Res 5 15224 PMID: 26477569

Yuan et al (2015) Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamox. resistance through cancer-associated fibroblast-derived fibronectin and PLoS One 17 69 PMID: 25990368

Carnesecchi et al (2015) Estrogens induce rapid cytoskeleton re-organization in human dermal fibroblasts via the non-classical receptor GPR30. Int J Mol Sci 10 e0120672 PMID: 25781607

Caballero et al (2017) Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol. Sci Rep 7 40981 PMID: 28112187

An et al (2014) Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. J Neurosci 15 10479 PMID: 24921706

Liu et al (2011) Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal mor. antinociception. J Neurosci 31 11836 PMID: 21849544

Cortes et al (2019) TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor. Oncogene 38 2910 PMID: 30575816

Cortes et al (2019) TAX mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival. EMBO Rep 20 PMID: 30538116

Cortes et al (2019) GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment. EMBO Rep 20 PMID: 30538117

Koong and Watson (2014) Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831

Bian et al (2019) 17β-E2 Regulates Glucose Metabolism and Ins. Secretion in Rat Islet β Cells Through GPER and Akt/mTOR/GLUT2 Pathway. Front Endocrinol (Lausanne) 10 531 PMID: 31447779

Loiola et al (2019) Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1. Front Endocrinol (Lausanne) 10 420 PMID: 31297095

Yi-Chen et al (2016) Estrogen and G protein-coupled estrogen receptor agonist G-1 cause relaxation of human gallbladder. Ci Ji Yi Xue Za Zhi 28 54-58 PMID: 28757722

Mazzuca et al (2015) Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat. J Pharmacol Exp Ther 352 291 PMID: 25472954

Lin et al (2021) GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERα-positive breast cancer cells. Aging (Albany NY) 13 16178-16197 PMID: 34182538

Christina et al (2021) The G-Protein-Coupled Estrogen Receptor (GPER) Regulates Trimethylation of Histone H3 at Lysine 4 and Represses Migration and Proliferation of Ovarian Cancer Cells In Vitro. Cells 10 PMID: 33799631

Bugel et al (2016) Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium. Toxicol Appl Pharmacol 296 31 PMID: 26908177

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G-15 as inhibitor of gper30 in rat endothelial cells.

By Anonymous on 01/04/2018

分析类型： In Vitro

种属： Rat

细胞系/组织： endothelial cell primary culture

i used to blocked the gper30 receptor in endothelial cell culture to quantificate if estradiol and metabolites induce mobilization of calcium

I order this product from chile

Pathways for G-15

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.