Catalog Number: 3678
Chemical Name: (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
Biological Activity
High affinity and selective GPER receptor antagonist (Ki = 20 nM) that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive and renoprotective effects of estrogen in vivo.
Technical Data
  • M.Wt:
    370.24
  • Formula:
    C19H16BrNO2
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    1161002-05-6
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. In vivo effects of a GPR30 antagonist.
    Dennis et al.
    Nat.Chem.Biol., 2009;5:421
  2. Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo.
    Hutchens et al.
    Am.J.Physiol.Renal Physiol., 2012;303:377
Citations:

The citations listed below are publications that use Tocris products. Selected citations for G-15 include:

9 Citations: Showing 1 - 9
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  1. Divergent regulation of ER and kiss genes by 17�-estradiol in hypothalamic ARC versus AVPV models.
    Authors: Treen Et al.
    Mol.Endocrinol. 2016;30:217
  2. HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol.
    Authors: Bertrand Et al.
    Mol Med Rep 2015;6:894
  3. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res 2015;5:15224
  4. 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.
    PLoS One 2015;17:69
  5. G-protein-coupled receptor 30-mediated antiapoptotic effect of estrogen on spinal motor neurons following injury and its underlying mechanisms.
    Authors: Chen Et al.
    Sci Rep 2015;12:1733
  6. Estrogens induce rapid cytoskeleton re-organization in human dermal fibroblasts via the non-classical receptor GPR30.
    Authors: Carnesecchi Et al.
    Int J Mol Sci 2015;10:e0120672
  7. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate 2014;74:1589
  8. Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor.
    Authors: An Et al.
    J Neurosci 2014;15:10479
  9. 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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