G-1

Tocris Bioscience, part of Bio-Techne | Catalog # 3577

COA / SDS

Potent and selective GPER agonist

Key Product Details

Description:	Potent and selective GPER agonist
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
Purity:	≥98% (HPLC)
Molecular Weight:	412.28

View Full Technical Details for G-1

Technical Data
Citations

Biological Activity for G-1

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.

Technical Data for G-1

M. Wt	412.28
Formula	C₂₁H₁₈BrNO₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	881639-98-1
PubChem ID	5322399
InChi Key	VHSVKVWHYFBIFJ-HKZYLEAXSA-N
Smiles	CC(C5=CC([C@@]4([H])[C@@]([H])3CC=C4)=C(C=C5)N[C@H]3[C@]1=CC(OCO2)=C2C=C1Br)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for G-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	41.23	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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Reconstitution Calculator

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References for G-1

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

G-1