G-1

Product Description

G-1 is a potent and selective GPER 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. Also inhibits glutamate-induced autophagy and neuronal loss in cultured primary cortical neurons.

Solubility

Preparing Stock Solutions for G-1

The following data is based on the product molecular weight 412.28

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.43 mL	12.13 mL	24.26 mL
5 mM	0.49 mL	2.43 mL	4.85 mL
10 mM	0.24 mL	1.21 mL	2.43 mL
50 mM	0.05 mL	0.24 mL	0.49 mL

Calculators

Background References

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

• Yue Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate. ACS Chem.Neurosci 2019 PMID: 31545891
• Bologa Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol.
• Blasko Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. J.Neuroimmunol. 2009 PMID: 19664827
• Ariazi The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res. 2010 PMID: 20086172
• Albanito G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17β-OE and selective GPR30 ligand G-1 in ovarian cancer cells. Cancer Res. 2007 PMID: 17308128