G-1

Cat. No. 3577 33 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Pricing	Availability		Qty

说明： Potent and selective GPER agonist

化学名： (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone

纯度： ≥98% (HPLC)

引用文献 (33)

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-1

G-1 is a potent and selective GPER agonist (K_i = 11 nM, EC₅₀ = 2 nM); displays no activity at ERα and ERβ at concentrations up to 10 μM. Increases cytosolic Ca²⁺ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC₅₀ values are 0.7 and 1.6 nM respectively) in vitro. Blocks MCF-1 cell cycle progression at the G₁ phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis. Also inhibits glutamate-induced autophagy and neuronal loss in cultured primary cortical neurons.

技术数据 for G-1

分子量	412.28
公式	C₂₁H₁₈BrNO₃
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	881639-98-1
PubChem ID	5322399
InChI Key	VHSVKVWHYFBIFJ-HKZYLEAXSA-N
Smiles	CC(C5=CC([C@@]4([H])[C@@]([H])3CC=C4)=C(C=C5)N[C@H]3[C@]1=CC(OCO2)=C2C=C1Br)=O

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-1

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	41.23	100

制备储备液 for G-1

以下数据基于产品分子量 412.28。 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
1 mM	2.43 mL	12.13 mL	24.26 mL
5 mM	0.49 mL	2.43 mL	4.85 mL
10 mM	0.24 mL	1.21 mL	2.43 mL
50 mM	0.05 mL	0.24 mL	0.49 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

产品说明书 for G-1

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-1

参考文献是支持产品生物活性的出版物。

Albanito et al (2007) G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-OE and selective GPR30 ligand G-1 in ovarian cancer cells. Cancer Res. 67 1859 PMID: 17308128

Blasko et al (2009) Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. J.Neuroimmunol. 214 67 PMID: 19664827

Ariazi et al (2010) The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res. 70 1184 PMID: 20086172

Bologa et al (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol. 2 207

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-1, please let us know.

按标靶查看相关产品

Estrogen (GPER) Receptors

按产品操作查看相关产品

查看全部 Estrogen (GPER) Receptor Agonists

关键词: G-1, G-1 supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER, Estrogen, (GPER), Receptors, 3577, Tocris Bioscience

33 篇 G-1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 G-1 的部分引用包括：

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

Bin et al (2020) G-protein-coupled estrogen receptor activation upregulates interleukin-1 receptor antagonist in the hippocampus after global cerebral ischemia: implications for neuronal self-defense. J Neuroinflammation 17 45 PMID: 32007102

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

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

Jamie et al (2020) Essential and sex-specific effects of mGluR5 in ventromedial hypothalamus regulating estrogen signaling and glucose balance. Proc Natl Acad Sci U S A 117 19566-19577 PMID: 32719118

Tzu-Ming et al (2020) Utilizing Designed Receptors Exclusively Activated by Designer Drug Chemogenetic Tools to Identify Beneficial G Protein-Coupled Receptor Signaling for Fibrosis. J Pharmacol Exp Ther 375 357-366 PMID: 32848074

Cláudio et al (2019) G protein-coupled estrogen receptor activates cell type-specific signaling pathways in cortical cultures: relevance to the selective loss of astrocytes. J Neurochem 149 27-40 PMID: 30570746

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

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

Huang et al (2016) GPR30 decreases with vascular aging and promotes vascular smooth muscle cells maintaining differentiated phenotype and suppressing migration via activation of ERK1/2. Onco Targets Ther 9 3415 PMID: 27354813

Chimento et al (2015) GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Cell Death Dis 6 19190 PMID: 26131713

Santolla et al (2015) SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer. Sci Rep 6 e1834 PMID: 26225773

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 Dis Model Mech 17 69 PMID: 25990368

Lappano et al (2015) A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models. Cell Death Dis 8 1237 PMID: 26183213

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

Nag and Mokha (2014) Activation of a Gq-coupled membrane estrogen receptor rapidly attenuates α2-adrenoceptor-induced antinociception via an ERK I/II-dependent, non-genomic mechanism in the female rat. Oncotarget 267 122 PMID: 24613724

Jing et al (2023) Anti-Inflammatory Actions of G-Protein-Coupled Estrogen Receptor 1 (GPER) and Brain-Derived Estrogen Following Cerebral Ischemia in Ovariectomized Rats. Biology (Basel) 12 PMID: 36671793

Meseke et al (2018) Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin. Eneuro 5 PMID: 30406178

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. Brain Behav 15 10479 PMID: 24921706

Anchan et al (2014) GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice. Am J Physiol Renal Physiol 4 51 PMID: 24653954

Chimento et al (2013) Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells. Int J Mol Sci 4 e747 PMID: 23907461

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

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

Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376 PMID: 24327954

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

Andrea et al (2021) Sex Differences in the Pro-Angiogenic Response of Human Endothelial Cells: Focus on PFKFB3 and FAK Activation. Front Pharmacol 11 587221 PMID: 33390959

Massimo et al (2021) ERα-independent NRF2-mediated immunoregulatory activity of tamoxifen. Biomed Pharmacother 144 112274 PMID: 34653752

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

您是否知道使用了 Tocris G-1 的优秀论文？请告知我们.

G-1 的评论

目前没有该产品的评论。 Be the first to review G-1 and earn rewards!

Have you used G-1?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Pathways for G-1

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.

G-1