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G-15

3678 21 Citations 1 Review Datasheet / COA / SDS
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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 (21)
Supplemental Products
Reviews (1)
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.

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Citations for G-15

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

21 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. GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment.
    Authors: Cortes Et al.
    EMBO Rep  2019;20
  3. TAX mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival.
    Authors: Cortes Et al.
    EMBO Rep  2019;20
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. Estrogen accelerates the resolution of inflammation in macrophagic cells.
    Authors: Villa Et al.
    Breast Cancer Res  2015;5:15224
  12. 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
  13. 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
  14. 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
  15. 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
  16. GPER mediates activation of HIF1α/VEGF signaling by estrogens.
    Authors: Francesco Et al.
    Cancer Res  2014;74:4053
  17. Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate  2014;74:1589
  18. 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
  19. 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
  20. 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
  21. 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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VersaClone cDNA Plasmids

Human GPER/GPR30 (NP_001496) VersaClone cDNA

RDC0352

Mouse GPER/GPR30 (NP_084047) VersaClone cDNA

RDC0390

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G-15 as inhibitor of gper30 in rat endothelial cells
By Anonymous on 01/04/2018
Application: Species: Rat

i used to blocked the gper30 receptor in endothelial cell culture to quantificate if estradiol and metabolites induce mobilization of calcium

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