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.
All Tocris products are intended for laboratory research use only.
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
Potent Smo antagonistONO 8130
EP1 receptor antagonistTC-G 1008
Potent and selective GPR39 agonistRo 1138452 hydrochloride
Selective prostacyclin IP receptor antagonistJNJ 27141491
Potent and selective human CCR2 antagonistTY 52156
S1P3 receptor antagonistElinogrel
P2Y12 antagonistRactopamine hydrochloride
Trace amine 1 (TA1) receptor agonist
September 6 - 9, 2015