G-15

Pricing Availability Delivery Time Qty
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 (9)
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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for G-15, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Estrogen (GPER) Receptor Antagonists

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

9 Citations for G-15

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

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

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

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

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

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


Do you know of a great paper that uses G-15 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

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.

Protocols

TODO: Add Protocols