G-15

Tocris Bioscience a Bio-Techne Brand

Catalog # 3678

Citations (21)

(1)

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Key Product Details

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)
Molecular Weight:	370.24

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Biological Activity for G-15

G-15 is a high affinity and selective GPER receptor antagonist (K_i = 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 for G-15

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	5.40 mL	27.01 mL	54.02 mL
2.5 mM	1.08 mL	5.40 mL	10.80 mL
5 mM	0.54 mL	2.70 mL	5.40 mL
25 mM	0.11 mL	0.54 mL	1.08 mL

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References for G-15

References are publications that support the biological activity of the product.

Yue Activation of G-protein-coupled receptor 30 protects neurons against excitotoxicity through inhibiting excessive autophagy induced by glutamate. ACS Chem.Neurosci. 2019 PMID: 31545891
Hutchens Estrogen protects renal endothelial barrier function from ischemia-reperfusion in vitro and in vivo. Am.J.Physiol.Renal Physiol. 2012 PMID: 22622457
Dennis In vivo effects of a GPR30 antagonist. Nat.Chem.Biol. 2009 PMID: 19430488

Citations for G-15 (21)

Showing 1 - 10 of 21 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for G-15 include:

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
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
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
Treen et al. (2016) Divergent regulation of ER and kiss genes by 17�-OE in hypothalamic ARC versus AVPV models. Mol.Endocrinol.. 30:217
PMID: 26726951
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
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
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
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 OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate. 74:1589
PMID: 25213831
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
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
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
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

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G-15 as inhibitor of gper30 in rat endothelial cells

Name: Anonymous

Species: Rat

Assay Type: In Vitro

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

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Product Documents for G-15

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.