G-1

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

COA / SDS

Potent and selective GPER agonist

Key Product Details

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%

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

Formula	C₂₁H₁₈BrNO₃
Storage	Store at -20°C
Purity	≥98%
CAS Number	881639-98-1

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

Solubility

Soluble Soluble to 100 mM in DMSO

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References for G-1

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

Lee E, Sidoryk-Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, Aschner M GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes. J Biol Chem, 2012;287(32):26817-28. 2012 PMID: 22645130
Chimento A, Sirianni R, Casaburi I, Ruggiero C, Maggiolini M, Ando S, Pezzi V 17 beta-Estradiol activates GPER- and ESR1-dependent pathways inducing apoptosis in GC-2 cells, a mouse spermatocyte-derived cell line. Mol. Cell. Endocrinol., 2012;355(1):49-59. 2012 PMID: 22306083
Tropea T, De Francesco E, Rigiracciolo D, Maggiolini M, Wareing M, Osol G, Mandala M Pregnancy Augments G Protein Estrogen Receptor (GPER) Induced Vasodilation in Rat Uterine Arteries via the Nitric Oxide - cGMP Signaling Pathway. PLoS ONE, 2015;10(11):e0141997. 2015 PMID: 26536245
P De Marco, R Lappano, EM Francesco, F Cirillo, M Pupo, S Avino, A Vivacqua, S Abonante, D Picard, M Maggiolini GPER signalling in both cancer-associated fibroblasts and breast cancer cells mediates a feedforward IL1?/IL1R1 response Sci Rep, 2016;6(0):24354. 2016 PMID: 27072893
Albanito et al. 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;67:1859 PMID: 17308128
Blasko et al. Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. J.Neuroimmunol., 2009;214:67 PMID: 19664827
Ariazi et al. The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer Res., 2010;70:1184 PMID: 20086172
Bologa et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol., 2006;2:207
Yue et al. Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate. ACS Chem.Neurosci, 2019;10:4227 PMID: 31545891

G-1

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

Key Product Details

Biological Activity for G-1

Technical Data for G-1

Solubility for G-1

Dilution Calculator

Reconstitution Calculator

References for G-1

Product Documents for G-1

COA

Certificate of Analysis

SDS

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