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G-1

Cat. No. 3577

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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 GPR30 receptor agonist (K_i = 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.

Licensing Information

Not for sale in the USA.

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.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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

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.

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.

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.

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Estrogen (GPR30) Receptors

Keywords: G-1, supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30

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