Catalog Number: 3577
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
Biological Activity
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis.
    Blasko et al.
    J.Neuroimmunol., 2009;214:67
  2. The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.
    Ariazi et al.
    Cancer Res., 2010;70:1184
  3. G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells.
    Albanito et al.
    Cancer Res., 2007;67:1859
  4. Virtual and biomolecular screening converge on a selective agonist for GPR30.
    Bologa et al.
    Nature Chem.Biol., 2006;2:207

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

Showing Results 1 - 10 of 11

  1. A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models.
    Authors: Lappano Et al.
    Cell Death Dis
  2. SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer.
    Authors: Santolla Et al.
    Sci Rep
  3. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo.
    Authors: Chimento Et al.
    Cell Death Dis
  4. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res
  5. Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamoxifen resistance through cancer-associated fibroblast-derived fibronectin and
    Authors: Yuan Et al.
    Dis Model Mech
  6. 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
  7. 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
  8. Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor.
    Authors: An Et al.
    Brain Behav
  9. Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells.
    Authors: Chimento Et al.
    Int J Mol Sci
  10. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
    Authors: Engelstoft Et al.
    Mol Metab
  11. 2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation.
    Authors: Duncan Et al.
    Proc Natl Acad Sci U S A
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