High affinity and selective GPER receptor antagonist (Ki = 20 nM) that displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive and renoprotective effects of estrogen in vivo.
|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 370.24. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.4 mL||27.01 mL||54.02 mL|
|2.5 mM||1.08 mL||5.4 mL||10.8 mL|
|5 mM||0.54 mL||2.7 mL||5.4 mL|
|25 mM||0.11 mL||0.54 mL||1.08 mL|
References are publications that support the biological activity of the product.
Dennis et al (2009) In vivo effects of a GPR30 antagonist. Nat.Chem.Biol. 5 421 PMID: 19430488
Hutchens et al (2012) Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo. Am.J.Physiol.Renal Physiol. 303 377 PMID: 22622457
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Keywords: G-15, G-15 supplier, high, affinity, selective, GPR30, antagonist, estrogen, oestrogen, receptors, GPER, Estrogen, (GPER), Receptors, 3678, Tocris Bioscience
15 Citations for G-15
Citations are publications that use Tocris products. Selected citations for G-15 include:
Bugel et al (2016) Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium. Toxicol Appl Pharmacol 296 31 PMID: 26908177
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
Koong and Watson (2014) Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951
Kanageswaran et al (2016) Modulatory Effects of Sex Steroids Progesterone and Estradiol on Odorant Evoked Responses in Olfactory Receptor Neurons. PLoS One 11 e0159640 PMID: 27494699
Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Mol Med Rep 6 894 PMID: 26441850
Chen et al (2015) G-protein-coupled receptor 30-mediated antiapoptotic effect of estrogen on spinal motor neurons following injury and its underlying mechanisms. Sci Rep 12 1733 PMID: 25872489
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 PLoS One 17 69 PMID: 25990368
Carnesecchi et al (2015) Estrogens induce rapid cytoskeleton re-organization in human dermal fibroblasts via the non-classical receptor GPR30. Int J Mol Sci 10 e0120672 PMID: 25781607
Francesco et al (2014) GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res 74 4053 PMID: 24894716
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
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
An et al (2014) Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. J Neurosci 15 10479 PMID: 24921706
Liu et al (2011) Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal morphine antinociception. J Neurosci 31 11836 PMID: 21849544
Do you know of a great paper that uses G-15 from Tocris? Please let us know.
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i used to blocked the gper30 receptor in endothelial cell culture to quantificate if estradiol and metabolites induce mobilization of calcium
I order this product from chile
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