G-1

Pricing Availability   Qty
Description: Potent and selective GPER agonist
Chemical Name: (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone
Purity: ≥98% (HPLC)
Datasheet
Citations (33)
Reviews
Pathways (1)

Biological Activity for G-1

G-1 is a potent and selective GPER agonist (Ki = 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.

Technical Data for G-1

M. Wt 412.28
Formula C21H18BrNO3
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for G-1

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.23 100

Preparing Stock Solutions for G-1

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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

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Product Datasheets for G-1

Certificate of Analysis / Product Datasheet
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References for G-1

References are publications that support the biological activity of the product.

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.

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Keywords: 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 Citations for G-1

Citations are publications that use Tocris products. Selected citations for G-1 include:

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


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Pathways for G-1

Estrogen Signaling Pathway

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.