G-1

Cat. No. 3577

G-1 C21H18BrNO3 [881639-98-1]

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Chemical Name: (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone

Biological Activity

Potent and selective GPER agonist (Ki = 11 nM, EC50 = 2 nM); displays no activity at ERα and ERβ at concentrations up to 10 μM. Increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro. Blocks MCF-1 cell cycle progression at the G1 phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis.

Technical Data

M.Wt:
412.28
Formula:
C21H18BrNO3
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
881639-98-1

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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Ariazi et al (2010) The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res. 70 1184. PMID: 20086172.

Blasko et al (2009) Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. J.Neuroimmunol. 214 67. PMID: 19664827.

Albanito et al (2007) G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells. Cancer Res. 67 1859. PMID: 17308128.

Bologa et al (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol. 2 207.

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Citations are publications that use Tocris products. Selected citations for G-1 include:

Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376. PMID: 24327954.

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.

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View Related Products by Product Action

Keywords: G-1, supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER, Tocris Bioscience, Estrogen (GPER) Receptor Agonist products

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