Catalog # Availability Size / Price Qty
G-1 | CAS No. 881639-98-1 | Estrogen and Related Receptor Agonists
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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%

Product Details
Citations (19)
Supplemental Products

Biological Activity

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

Soluble to 100 mM in DMSO
Store at -20°C

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.

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Citations for G-1

The citations listed below are publications that use Tocris products. Selected citations for G-1 include:

19 Citations: Showing 1 - 10

  1. TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor.
    Authors: Cortes Et al.
    Oncogene  2019;38:2910
  2. Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1.
    Authors: Loiola Et al.
    Front Endocrinol (Lausanne)  2019;10:420
  3. Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin.
    Authors: Meseke Et al.
    Eneuro  2018;5
  4. Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol.
    Authors: Caballero Et al.
    Sci Rep  2017;7:40981
  5. GPR30 decreases with vascular aging and promotes vascular smooth muscle cells maintaining differentiated phenotype and suppressing migration via activation of ERK1/2.
    Authors: Huang Et al.
    Onco Targets Ther  2016;9:3415
  6. A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models.
    Authors: Lappano Et al.
    Cell Death Dis  2015;8:1237
  7. SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer.
    Authors: Santolla Et al.
    Sci Rep  2015;6:e1834
  8. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo.
    Authors: Chimento Et al.
    Cell Death Dis  2015;6:19190
  9. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res  2015;5:15224
  10. Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat.
    Authors: Mazzuca Et al.
    J Pharmacol Exp Ther  2015;352:291
  11. 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
    Authors: Yuan Et al.
    Dis Model Mech  2015;17:69
  12. GPER mediates activation of HIF1α/VEGF signaling by estrogens.
    Authors: Francesco Et al.
    Cancer Res  2014;74:4053
  13. GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice.
    Authors: Anchan Et al.
    Am J Physiol Renal Physiol  2014;4:51
  14. Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility.
    Authors: Sandner Et al.
    Andrology  2014;2:695
  15. 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.
    Authors: Nag and Mokha
    Oncotarget  2014;267:122
  16. Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor.
    Authors: An Et al.
    Brain Behav  2014;15:10479
  17. Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells.
    Authors: Chimento Et al.
    Int J Mol Sci  2013;4:e747
  18. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
    Authors: Engelstoft Et al.
    Mol Metab  2013;2:376
  19. 2-MethoxyOE inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation.
    Authors: Duncan Et al.
    Proc Natl Acad Sci U S A  2012;109:21034


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