Cat. No. 3577
Chemical Name: (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,
Biological ActivityPotent and selective GPR30 receptor 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: G-1, supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER
Find multiple products by catalog number
New Products in this Area
FFA1 (GPR40) antagonistAR-C 118925XX
Selective, competitive P2Y2 receptor antagonistNIBR 189
Potent and selective EBI2 (GPR183) receptor antagonistONO AE3 208
High affinity and selective EP4 antagonistTCS 3035
GPR35 agonistPF 5274857 hydrochloride
Potent and selective Smoothened (Smo) receptor antagonistGSK 137647
Potent and selective FFA4 (GPR120) agonistAH 7614
Selective FFA4 (GPR120) antagonist
One Day Symposium
March 17, 2015