Potent 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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
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|
References are publications that support the biological activity of the product.
Albanito et al (2007) 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. 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
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 G-1, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: G-1, G-1 supplier, Potent, selective, G1, GPR30, agonists, receptors, estrogen, oestrogen, G, protein-coupled, receptor, 30, GPER, Estrogen, (GPER), Receptors, 3577, Tocris Bioscience
14 Citations for G-1
Citations are publications that use Tocris products. Selected citations for G-1 include:
An et al (2014) Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. Brain Behav 15 10479 PMID: 24921706
Anchan et al (2014) GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice. Am J Physiol Renal Physiol 4 51 PMID: 24653954
Chimento et al (2013) Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells. Int J Mol Sci 4 e747 PMID: 23907461
Chimento et al (2015) GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Cell Death Dis 6 19190 PMID: 26131713
Santolla et al (2015) SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer. Sci Rep 6 e1834 PMID: 26225773
Villa et al (2015) Estrogen accelerates the resolution of inflammation in macrophagic cells. Breast Cancer Res 5 15224 PMID: 26477569
Yuan et al (2015) Acquisition of epithelial-mesenchymal transition phenotype in the tamoxifen-resistant breast cancer cell: a new role for G protein-coupled estrogen receptor in mediating tamoxifen resistance through cancer-associated fibroblast-derived fibronectin and Dis Model Mech 17 69 PMID: 25990368
Lappano et al (2015) A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models. Cell Death Dis 8 1237 PMID: 26183213
Francesco et al (2014) GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res 74 4053 PMID: 24894716
Nag and Mokha (2014) Activation of a Gq-coupled membrane estrogen receptor rapidly attenuates α2-adrenoceptor-induced antinociception via an ERK I/II-dependent, non-genomic mechanism in the female rat. Oncotarget 267 122 PMID: 24613724
Sandner et al (2014) Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility. Andrology 2 695 PMID: 25052196
Duncan et al (2012) 2-MethoxyOE inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A 109 21034 PMID: 23213242
Mazzuca et al (2015) Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat. J Pharmacol Exp Ther 352 291 PMID: 25472954
Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376 PMID: 24327954
Do you know of a great paper that uses G-1 from Tocris? Please let us know.
Reviews for G-1
There are currently no reviews for this product. Be the first to review G-1 and earn rewards!
Have you used G-1?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.