G-1

  ( 13 citations )    
Product Datasheet
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
Product Details
Citations (13)
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Reviews
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:
    412.28
  • Formula:
    C21H18BrNO3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98
  • Storage:
    Store at -20°C
  • CAS No:
    881639-98-1
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.
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Citations:

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

13 Citations: Showing 1 - 10
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  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  2015;8:1237
  2. SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer.
    Authors: Santolla Et al.
    Sci Rep  2015;6:e1834
  3. 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
  4. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res  2015;5:15224
  5. 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
  6. 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  2015;17:69
  7. 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
  8. 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
  9. 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
  10. 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
  11. Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells.
    Authors: Chimento Et al.
    Int J Mol Sci  2013;4:e747
  12. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells.
    Authors: Engelstoft Et al.
    Mol Metab  2013;2:376
  13. 2-Methoxyestradiol 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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