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G-15

Catalog #: 3678
31 Citations Datasheet
Catalog # Availability Size / Price Qty
3678/10
G-15 | CAS No. 1161002-05-6 | Estrogen and Related Receptor Antagonists
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Description: High affinity and selective GPER antagonist

Chemical Name: (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline

Purity: ≥99%

Product Details
Citations (31)
Supplemental Products
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

G-15 is a 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Pregnancy Augments G Protein Estrogen Receptor (GPER) Induced Vasodilation in Rat Uterine Arteries via the Nitric Oxide - cGMP Signaling Pathway.
    Tropea T, De Francesco E, Rigiracciolo D, Maggiolini M, Wareing M, Osol G, Mandala M
    PLoS ONE, 2015;10(11):e0141997.
  2. GPER signalling in both cancer-associated fibroblasts and breast cancer cells mediates a feedforward IL1?/IL1R1 response
    P De Marco, R Lappano, EM Francesco, F Cirillo, M Pupo, S Avino, A Vivacqua, S Abonante, D Picard, M Maggiolini
    Sci Rep, 2016;6(0):24354.
  3. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes.
    Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M
    J Biol Chem, 2012;287(32):26817-28.
  4. 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
  5. In vivo effects of a GPR30 antagonist.
    Dennis et al.
    Nat.Chem.Biol., 2009;5:421
  6. Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate.
    Yue et al.
    ACS Chem.Neurosci, 2019;10:4227
  7. Ginsenoside Rb1 Prevents Dysfunction of Endothelial Cells by Suppressing Inflammatory Response and Apoptosis in the High-Fat Diet Plus Balloon Catheter-Injured Rabbit Model via the G Protein-Coupled Estrogen Receptor-Mediated Phosphatidylinositol 3-Kinases (PI3K)/Akt Pathway
    G Yang, J Zhuo, Y Lin, M Zhang, L Liu, X Chen, R Gao
    Med. Sci. Monit., 2019;25(0):7407-7417.

Product Datasheets

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Citations for G-15

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

31 Citations: Showing 1 - 10

  1. Nuclear and Membrane Receptors for Sex Steroids Are Involved in the Regulation of Delta/Serrate/LAG-2 Proteins in Rodent Sertoli Cells.
    Authors: Alicja Et al.
    Int J Mol Sci  2022;23
  2. GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERα-positive breast cancer cells.
    Authors: Lin Et al.
    Aging (Albany NY)  2021;13:16178-16197
  3. The G-Protein-Coupled Estrogen Receptor (GPER) Regulates Trimethylation of Histone H3 at Lysine 4 and Represses Migration and Proliferation of Ovarian Cancer Cells In Vitro.
    Authors: Christina Et al.
    Cells  2021;10
  4. G Protein-Coupled Estrogen Receptor Regulates Actin Cytoskeleton Dynamics to Impair Cell Polarization.
    Authors: Stephen D Et al.
    Front Cell Dev Biol  2020;8:592628
  5. G Protein-Coupled Estrogen Receptor Mediates Cell Proliferation through the cAMP/PKA/CREB Pathway in Murine Bone Marrow Mesenchymal Stem Cells.
    Authors: Mei-Ling Et al.
    Int J Mol Sci  2020;21
  6. GPER Activation Inhibits Cancer Cell Mechanotransduction and Basement Membrane Invasion via RhoA.
    Authors: David A Et al.
    Cancers (Basel)  2020;12
  7. Low-dose Bisphenol-A regulates inflammatory cytokines through GPR30 in mammary adipose cells.
    Authors: Francesco Et al.
    J Mol Endocrinol  2019;63:273-283
  8. TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor.
    Authors: Cortes Et al.
    Oncogene  2019;38:2910
  9. GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment.
    Authors: Cortes Et al.
    EMBO Rep  2019;20
  10. TAX mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival.
    Authors: Cortes Et al.
    EMBO Rep  2019;20
  11. 17β-E2 Regulates Glucose Metabolism and Ins. Secretion in Rat Islet β Cells Through GPER and Akt/mTOR/GLUT2 Pathway.
    Authors: Bian Et al.
    Front Endocrinol (Lausanne)  2019;10:531
  12. 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
  13. 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
  14. Divergent regulation of ER and kiss genes by 17�-OE in hypothalamic ARC versus AVPV models.
    Authors: Treen Et al.
    Mol.Endocrinol.  2016;30:217
  15. Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium.
    Authors: Bugel Et al.
    Toxicol Appl Pharmacol  2016;296:31
  16. Estrogen and G protein-coupled estrogen receptor agonist G-1 cause relaxation of human gallbladder.
    Authors: Yi-Chen Et al.
    Ci Ji Yi Xue Za Zhi  2016;28:54-58
  17. Modulatory Effects of Sex Steroids Progesterone and OE on Odorant Evoked Responses in Olfactory Receptor Neurons.
    Authors: Kanageswaran Et al.
    PLoS One  2016;11:e0159640
  18. 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
  19. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res  2015;5:15224
  20. 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
  21. 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.
    PLoS One  2015;17:69
  22. 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
  23. 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
  24. GPER mediates activation of HIF1α/VEGF signaling by estrogens.
    Authors: Francesco Et al.
    Cancer Res  2014;74:4053
  25. Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate  2014;74:1589
  26. 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
  27. Activation of membrane estrogen receptors attenuates opioid receptor-like1 receptor-mediated antinociception via an ERK-dependent non-genomic mechanism.
    Authors: S Et al.
    Neuroscience  2014;255:177-90
  28. 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
  29. GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer.
    Authors: Manran Et al.
    Breast Cancer Res  2013;15:R114
  30. 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
  31. Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal mor. antinociception.
    Authors: Liu Et al.
    J Neurosci  2011;31:11836

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