Cat. No. 3577
Chemical Name: (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,
Biological ActivityPotent and selective GPER 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
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.
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.
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.
Bologa et al (2006) Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chem.Biol. 2 207.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for G-1 include:
Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376. PMID: 24327954.
Duncan et al (2012) 2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A 109 21034. PMID: 23213242.
Do you know of a great paper that uses G-1 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: G-1, supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER, Tocris Bioscience, Estrogen (GPER) Receptor Agonist products
Find multiple products by catalog number
New Products in this Area
Potent P2Y12 antagonist; cell permeableA 971432
Potent and selective S1P5 agonistGLPG 0974
Potent FFA2 antagonistOgerin
Selective positive allosteric modulator at GPR68BGC 20-1531 hydrochloride
High affinity and selective EP4 antagonistMontelukast sodium
CysLT1 antagonistBeraprost sodium
Potent prostacyclin IP receptor agonistJNJ 63533054
Potent and selective GPR139 agonist
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.