G-15

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Cat.No. 3678 - G-15 | C19H16BrNO2 | CAS No. 1161002-05-6
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% (HPLC)
Datasheet
Citations (15)
Reviews (1)
Literature
Pathways

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
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1161002-05-6
PubChem ID 90488870
InChI Key LBBDCJLRQXMUAE-FWHYVADDSA-N
Smiles BrC1=CC4=C(OCO4)C=[C@@]1[C@@H]2NC(C=CC=C5)=C5[C@@]3([H])[C@@]([H])2CC=C3.BrC6=CC9=C(OCO9)C=[C@@]6[C@H]7NC(C=CC=C%10)=C%10[C@]8([H])[C@]([H])7CC=C8

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.51 50

Preparing Stock Solutions

The following data is based on the product molecular weight 370.24. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.7 mL 13.5 mL 27.01 mL
5 mM 0.54 mL 2.7 mL 5.4 mL
10 mM 0.27 mL 1.35 mL 2.7 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Dennis et al (2009) In vivo effects of a GPR30 antagonist. Nat.Chem.Biol. 5 421 PMID: 19430488

Hutchens et al (2012) Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo. Am.J.Physiol.Renal Physiol. 303 377 PMID: 22622457


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View all Estrogen (GPER) Receptor Antagonists

Keywords: G-15, G-15 supplier, high, affinity, selective, GPR30, antagonist, estrogen, oestrogen, receptors, GPER, Estrogen, (GPER), Receptors, 3678, Tocris Bioscience

15 Citations for G-15

Citations are publications that use Tocris products. Selected citations for G-15 include:

An et al (2014) Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. J Neurosci 15 10479 PMID: 24921706

Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Mol Med Rep 6 894 PMID: 26441850

Chen et al (2015) G-protein-coupled receptor 30-mediated antiapoptotic effect of estrogen on spinal motor neurons following injury and its underlying mechanisms. Sci Rep 12 1733 PMID: 25872489

Villa et al (2015) Estrogen accelerates the resolution of inflammation in macrophagic cells. Breast Cancer Res 5 15224 PMID: 26477569

Yuan et al (2015) 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 PLoS One 17 69 PMID: 25990368

Carnesecchi et al (2015) Estrogens induce rapid cytoskeleton re-organization in human dermal fibroblasts via the non-classical receptor GPR30. Int J Mol Sci 10 e0120672 PMID: 25781607

Duncan et al (2012) 2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A 109 21034 PMID: 23213242

Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951

Sandner et al (2014) Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility. Andrology 2 695 PMID: 25052196

Francesco et al (2014) GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res 74 4053 PMID: 24894716

Bugel et al (2016) Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium. Toxicol Appl Pharmacol 296 31 PMID: 26908177

Kanageswaran et al (2016) Modulatory Effects of Sex Steroids Progesterone and Estradiol on Odorant Evoked Responses in Olfactory Receptor Neurons. PLoS One 11 e0159640 PMID: 27494699

Mazzuca et al (2015) Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat. J Pharmacol Exp Ther 352 291 PMID: 25472954

Koong and Watson (2014) Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831

Liu et al (2011) Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal morphine antinociception. J Neurosci 31 11836 PMID: 21849544


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Reviews for G-15

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G-15 as inhibitor of gper30 in rat endothelial cells
By Anonymous on 01/04/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: endothelial cell primary culture

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

I order this product from chile


Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling

Pathways for G-15

Estrogen

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.