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Description: High affinity and selective GPER antagonist
Chemical Name: (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
Purity: ≥99% (HPLC)
Biological Activity for G-15
G-15 is a 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.
Technical Data for G-15
| M. Wt | 370.24 |
| Formula | C19H16BrNO2 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1161002-05-6 |
| PubChem ID | 90488870 |
| InChI Key | LBBDCJLRQXMUAE-FWHYVADDSA-N |
| Smiles | BrC1=CC4=C(OCO4)C=[C@@]1[C@@H]2NC(C=CC=C5)=C5[C@@]3([H])[C@@]([H])2CC=C3.BrC6=CC9=C(OCO9)C=[C@@]6[C@H]7NC(C=CC=C%10)=C%10[C@]8([H])[C@]([H])7CC=C8 |
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.
Solubility Data for G-15
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.51 | 50 |
Preparing Stock Solutions for G-15
The following data is based on the product molecular weight 370.24. 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 |
|---|---|---|---|
| 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 |
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Product Datasheets for G-15
References for G-15
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
Yue et al (2019) Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate. ACS Chem.Neurosci. 10 4227 PMID: 31545891
If you know of a relevant reference for G-15, please let us know.
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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
31 Citations for G-15
Citations are publications that use Tocris products. Selected citations for G-15 include:
Lin et al (2021) GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERα-positive breast cancer cells. Aging (Albany NY) 13 16178-16197 PMID: 34182538
Christina et al (2021) The G-Protein-Coupled Estrogen Receptor (GPER) Regulates Trimethylation of Histone H3 at Lysine 4 and Represses Migration and Proliferation of Ovarian Cancer Cells In Vitro. Cells 10 PMID: 33799631
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
Alicja et al (2022) Nuclear and Membrane Receptors for Sex Steroids Are Involved in the Regulation of Delta/Serrate/LAG-2 Proteins in Rodent Sertoli Cells. Int J Mol Sci 23 PMID: 35216398
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
S et al (2014) Activation of membrane estrogen receptors attenuates opioid receptor-like1 receptor-mediated antinociception via an ERK-dependent non-genomic mechanism. Neuroscience 255 177-90 PMID: 24452062
Manran et al (2013) GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer. Breast Cancer Res 15 R114 PMID: 24289103
Stephen D et al (2020) G Protein-Coupled Estrogen Receptor Regulates Actin Cytoskeleton Dynamics to Impair Cell Polarization. Front Cell Dev Biol 8 592628 PMID: 33195261
Mei-Ling et al (2020) G Protein-Coupled Estrogen Receptor Mediates Cell Proliferation through the cAMP/PKA/CREB Pathway in Murine Bone Marrow Mesenchymal Stem Cells. Int J Mol Sci 21 PMID: 32899453
David A et al (2020) GPER Activation Inhibits Cancer Cell Mechanotransduction and Basement Membrane Invasion via RhoA. Cancers (Basel) 12 PMID: 31991740
Francesco et al (2019) Low-dose Bisphenol-A regulates inflammatory cytokines through GPR30 in mammary adipose cells. J Mol Endocrinol 63 273-283 PMID: 31546233
Kanageswaran et al (2016) Modulatory Effects of Sex Steroids Progesterone and OE on Odorant Evoked Responses in Olfactory Receptor Neurons. PLoS One 11 e0159640 PMID: 27494699
Francesco et al (2014) GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res 74 4053 PMID: 24894716
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
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -OE 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
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 tamox. 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
Caballero et al (2017) Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol. Sci Rep 7 40981 PMID: 28112187
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 mor. antinociception. J Neurosci 31 11836 PMID: 21849544
Cortes et al (2019) TAX mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor. Oncogene 38 2910 PMID: 30575816
Cortes et al (2019) TAX mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival. EMBO Rep 20 PMID: 30538116
Cortes et al (2019) GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment. EMBO Rep 20 PMID: 30538117
Koong and Watson (2014) Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831
Bian et al (2019) 17β-E2 Regulates Glucose Metabolism and Ins. Secretion in Rat Islet β Cells Through GPER and Akt/mTOR/GLUT2 Pathway. Front Endocrinol (Lausanne) 10 531 PMID: 31447779
Loiola et al (2019) Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1. Front Endocrinol (Lausanne) 10 420 PMID: 31297095
Yi-Chen et al (2016) Estrogen and G protein-coupled estrogen receptor agonist G-1 cause relaxation of human gallbladder. Ci Ji Yi Xue Za Zhi 28 54-58 PMID: 28757722
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
Do you know of a great paper that uses G-15 from Tocris? Please let us know.
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G-15 as inhibitor of gper30 in rat endothelial cells.
By
Anonymous on 01/04/2018
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: endothelial cell primary culture
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
Pathways for G-15
