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company name :
Tocris Bioscience
product type :
chemical
product name :
G-15
catalog :
3678/10
quantity :
10 mg
price :
277 USD
more info or order :
citations: 35
Reference
Lustofin S, Kami x144 ska A, Brzoskwinia M, Cyran J, Kotula Balak M, Bili x144 ska B, et al. 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. 2022;23: pubmed publisher
Liu L, Liu S, Luo H, Chen C, Zhang X, He L, et al. GPR30-mediated HMGB1 upregulation in CAFs induces autophagy and tamoxifen resistance in ERα-positive breast cancer cells. Aging (Albany NY). 2021;13:16178-16197 pubmed publisher
Han N, Heublein S, Jeschke U, Kuhn C, Hester A, Czogalla B, et al. 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. 2021;10: pubmed publisher
Lachowski D, Cortés E, Matellan C, Rice A, Lee D, Thorpe S, et al. G Protein-Coupled Estrogen Receptor Regulates Actin Cytoskeleton Dynamics to Impair Cell Polarization. Front Cell Dev Biol. 2020;8:592628 pubmed publisher
Chuang S, Chen C, Chou Y, Ho M, Chang J. 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. 2020;21: pubmed publisher
Rice A, Cortés E, Lachowski D, Oertle P, Matellan C, Thorpe S, et al. GPER Activation Inhibits Cancer Cell Mechanotransduction and Basement Membrane Invasion via RhoA. Cancers (Basel). 2020;12: pubmed publisher
Yang G, Zhuo J, Lin Y, Zhang M, Liu L, Chen X, et al. Ginsenoside Rb1 Prevents Dysfunction of Endothelial Cells by Suppressing Inflammatory Response and Apoptosis in the High-Fat Diet Plus Balloon Catheter-Injured Rabbit Model via the G Protein-Coupled Estrogen Receptor-Mediated Phosphatidylinositol 3-K. Med Sci Monit. 2019;25:7407-7417 pubmed publisher
Cimmino I, Oriente F, D Esposito V, Liguoro D, Liguoro P, Ambrosio M, et al. Low-dose Bisphenol-A regulates inflammatory cytokines through GPR30 in mammary adipose cells. J Mol Endocrinol. 2019;63:273-283 pubmed publisher
Bian C, Bai B, Gao Q, Li S, Zhao Y. 17β-Estradiol Regulates Glucose Metabolism and Insulin Secretion in Rat Islet β Cells Through GPER and Akt/mTOR/GLUT2 Pathway. Front Endocrinol (Lausanne). 2019;10:531 pubmed publisher
Loiola R, Wickstead E, Solito E, McArthur S. Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1. Front Endocrinol (Lausanne). 2019;10:420 pubmed publisher
Cortés E, Lachowski D, Rice A, Thorpe S, Robinson B, Yeldag G, et al. Tamoxifen mechanically deactivates hepatic stellate cells via the G protein-coupled estrogen receptor. Oncogene. 2019;38:2910-2922 pubmed publisher
Cortés E, Sarper M, Robinson B, Lachowski D, Chronopoulos A, Thorpe S, et al. GPER is a mechanoregulator of pancreatic stellate cells and the tumor microenvironment. EMBO Rep. 2019;20: pubmed publisher
Cortés E, Lachowski D, Robinson B, Sarper M, Teppo J, Thorpe S, et al. Tamoxifen mechanically reprograms the tumor microenvironment via HIF-1A and reduces cancer cell survival. EMBO Rep. 2019;20: pubmed publisher
Lee M, Yang Y, Chen Y, Chang B, Li Y, Huang S. Estrogen and G protein-coupled estrogen receptor agonist G-1 cause relaxation of human gallbladder. Ci Ji Yi Xue Za Zhi. 2016;28:54-58 pubmed publisher
Caballero I, Boyd J, Almiñana C, Sánchez López J, Basatvat S, Montazeri M, et al. Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol. Sci Rep. 2017;7:40981 pubmed publisher
Kanageswaran N, Nagel M, Scholz P, Mohrhardt J, Gisselmann G, Hatt H. Modulatory Effects of Sex Steroids Progesterone and Estradiol on Odorant Evoked Responses in Olfactory Receptor Neurons. PLoS ONE. 2016;11:e0159640 pubmed publisher
De Marco P, Lappano R, De Francesco E, Cirillo F, Pupo M, Avino S, et al. GPER signalling in both cancer-associated fibroblasts and breast cancer cells mediates a feedforward IL1?/IL1R1 response. Sci Rep. 2016;6:24354 pubmed publisher
Bugel S, Wehmas L, La Du J, Tanguay R. Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium. Toxicol Appl Pharmacol. 2016;296:31-41 pubmed publisher
Treen A, Luo V, Chalmers J, Dalvi P, Tran D, Ye W, et al. Divergent Regulation of ER and Kiss Genes by 17β-Estradiol in Hypothalamic ARC Versus AVPV Models. Mol Endocrinol. 2016;30:217-33 pubmed publisher
Tropea T, De Francesco E, Rigiracciolo D, Maggiolini M, Wareing M, Osol G, et al. Pregnancy Augments G Protein Estrogen Receptor (GPER) Induced Vasodilation in Rat Uterine Arteries via the Nitric Oxide - cGMP Signaling Pathway. PLoS ONE. 2015;10:e0141997 pubmed publisher
Villa A, Rizzi N, Vegeto E, Ciana P, Maggi A. Estrogen accelerates the resolution of inflammation in macrophagic cells. Sci Rep. 2015;5:15224 pubmed publisher
Bertrand S, Hu C, Aksenova M, Mactutus C, Booze R. HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Front Microbiol. 2015;6:894 pubmed publisher
Yuan J, Liu M, Yang L, Tu G, Zhu Q, Chen M, et al. 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 an. Breast Cancer Res. 2015;17:69 pubmed publisher
Chen J, Hu R, Ge H, Duanmu W, Li Y, Xue X, et al. G-protein-coupled receptor 30-mediated antiapoptotic effect of estrogen on spinal motor neurons following injury and its underlying mechanisms. Mol Med Rep. 2015;12:1733-40 pubmed publisher
Carnesecchi J, Malbouyres M, de Mets R, Balland M, Beauchef G, Vié K, et al. Estrogens induce rapid cytoskeleton re-organization in human dermal fibroblasts via the non-classical receptor GPR30. PLoS ONE. 2015;10:e0120672 pubmed publisher
Mazzuca M, Mata K, Li W, Rangan S, Khalil R. Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat. J Pharmacol Exp Ther. 2015;352:291-304 pubmed publisher
Koong L, Watson C. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate. 2014;74:1589-603 pubmed publisher
Sandner F, Welter H, Schwarzer J, Kohn F, Urbanski H, Mayerhofer A. Expression of the oestrogen receptor GPER by testicular peritubular cells is linked to sexual maturation and male fertility. Andrology. 2014;2:695-701 pubmed publisher
An G, Li W, Yan T, Li S. Estrogen rapidly enhances incisional pain of ovariectomized rats primarily through the G protein-coupled estrogen receptor. Int J Mol Sci. 2014;15:10479-91 pubmed publisher
De Francesco E, Pellegrino M, Santolla M, Lappano R, Ricchio E, Abonante S, et al. GPER mediates activation of HIF1α/VEGF signaling by estrogens. Cancer Res. 2014;74:4053-64 pubmed publisher
Small K, Nag S, Mokha S. Activation of membrane estrogen receptors attenuates opioid receptor-like1 receptor-mediated antinociception via an ERK-dependent non-genomic mechanism. Neuroscience. 2013;255:177-90 pubmed publisher
Mo Z, Liu M, Yang F, Luo H, Li Z, Tu G, et al. GPR30 as an initiator of tamoxifen resistance in hormone-dependent breast cancer. Breast Cancer Res. 2013;15:R114 pubmed publisher
Duncan G, Brenner D, Tusche M, Brüstle A, Knobbe C, Elia A, et al. 2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation. Proc Natl Acad Sci U S A. 2012;109:21034-9 pubmed publisher
Lee E, Sidoryk Wegrzynowicz M, Wang N, Webb A, Son D, Lee K, et al. GPR30 regulates glutamate transporter GLT-1 expression in rat primary astrocytes. J Biol Chem. 2012;287:26817-28 pubmed publisher
Liu N, Chakrabarti S, Schnell S, Wessendorf M, Gintzler A. Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal ?- and ?-opioid receptor heterodimerization and female-specific spinal morphine antinociception. J Neurosci. 2011;31:11836-45 pubmed publisher
image
image 1 :
Tocris Bioscience 3678/10 image 1
Cat.No. 3678 - G-15 C19H16BrNO2 CAS No. 1161002-05-6
product information
brand :
Tocris, a Bio-Techne brand
catalog number base :
3678
SKU :
3678/10
product name :
G-15
description :
High affinity and selective GPER antagonist
target :
Estrogen and Related Receptor Antagonists
unit size :
10 mg
category :
Small Molecules
purity :
99%
storage :
Store at -20°C
observed molecular weight :
370.24
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
G-15 is a high affinity and selective GPER receptor antagonist (Ki = 20 nM) that displays no affinity for ER and ER at concentrations up to 10 M. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive and renoprotective effects of estrogen in vivo .
product keywords :
high affinity selective GPR30 antagonist estrogen oestrogen receptors GPER Estrogen (GPER) Receptors 3678,
extended description :
High affinity and selective GPER antagonist
chemical name text :
(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
formula :
C19H16BrNO2
formula text :
C19H16BrNO2
cas num :
1161002-05-6
USD :
268
USD 2025 :
277 USD
product details :
High affinity and selective GPER antagonist
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK