Cat. No. 3678
Chemical Name: (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benz
Biological ActivityHigh 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.
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 / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
Dennis et al (2009) In vivo effects of a GPR30 antagonist. Nat.Chem.Biol. 5 421. PMID: 19430488.
If you know of a relevant reference for G-15 please let us know.
Citations are publications that use Tocris products. Selected citations for G-15 include:
Treen et al (2016) Divergent regulation of ER and kiss genes by 17ß-estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217. PMID: 26726951.
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.
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.
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 β1-integrin signaling pathway in tumor cells. PLoS One 17 69. PMID: 25990368.
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.
Koong and Watson (2014) Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589. PMID: 25213831.
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.
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Keywords: G-15, supplier, high, affinity, selective, GPR30, antagonist, estrogen, oestrogen, receptors, GPER, Tocris Bioscience, Estrogen (GPER) Receptor Antagonist products
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