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company name :
Tocris Bioscience
product type :
chemical
product name :
3577/10
catalog :
3577/10
quantity :
10 mg
price :
276 USD
more info or order :
citations: 37
Reference
Xu J, Bai J, Gao F, Xu C, Huang Y, Li D, et al. Anti-Inflammatory Actions of G-Protein-Coupled Estrogen Receptor 1 (GPER) and Brain-Derived Estrogen Following Cerebral Ischemia in Ovariectomized Rats. Biology (Basel). 2023;12: pubmed publisher
Pepe G, Sfogliarini C, Rizzello L, Battaglia G, Pinna C, Rovati G, et al. ERα-independent NRF2-mediated immunoregulatory activity of tamoxifen. Biomed Pharmacother. 2021;144:112274 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
Boscaro C, Trenti A, Baggio C, Scapin C, Trevisi L, Cignarella A, et al. Sex Differences in the Pro-Angiogenic Response of Human Endothelial Cells: Focus on PFKFB3 and FAK Activation. Front Pharmacol. 2020;11:587221 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
Zhang J, Vardy E, Muise E, Wang T, Visconti R, Vadlamudi A, et al. Utilizing Designed Receptors Exclusively Activated by Designer Drug Chemogenetic Tools to Identify Beneficial G Protein-Coupled Receptor Signaling for Fibrosis. J Pharmacol Exp Ther. 2020;375:357-366 pubmed publisher
Fagan M, Ameroso D, Meng A, Rock A, Maguire J, Rios M. Essential and sex-specific effects of mGluR5 in ventromedial hypothalamus regulating estrogen signaling and glucose balance. Proc Natl Acad Sci U S A. 2020;117:19566-19577 pubmed publisher
Bai N, Zhang Q, Zhang W, Liu B, Yang F, Brann D, et al. G-protein-coupled estrogen receptor activation upregulates interleukin-1 receptor antagonist in the hippocampus after global cerebral ischemia: implications for neuronal self-defense. J Neuroinflammation. 2020;17:45 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
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
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
Roque C, Mendes Oliveira J, Baltazar G. G protein-coupled estrogen receptor activates cell type-specific signaling pathways in cortical cultures: relevance to the selective loss of astrocytes. J Neurochem. 2019;149:27-40 pubmed publisher
Meseke M, Neumüller F, Brunne B, Li X, Anstötz M, Pohlkamp T, et al. Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin. Eneuro. 2018;5: 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
Huang F, Yin J, Li K, Li Y, Qi H, Fang L, et al. GPR30 decreases with vascular aging and promotes vascular smooth muscle cells maintaining differentiated phenotype and suppressing migration via activation of ERK1/2. Onco Targets Ther. 2016;9:3415-22 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
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
Santolla M, Avino S, Pellegrino M, De Francesco E, De Marco P, Lappano R, et al. SIRT1 is involved in oncogenic signaling mediated by GPER in breast cancer. Cell Death Dis. 2015;6:e1834 pubmed publisher
Lappano R, Rosano C, Pisano A, Santolla M, De Francesco E, De Marco P, et al. A calixpyrrole derivative acts as an antagonist to GPER, a G-protein coupled receptor: mechanisms and models. Dis Model Mech. 2015;8:1237-46 pubmed publisher
Chimento A, Sirianni R, Casaburi I, Zolea F, Rizza P, Avena P, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015;6:19190-203 pubmed
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
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
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
Anchan D, Clark S, Pollard K, Vasudevan N. GPR30 activation decreases anxiety in the open field test but not in the elevated plus maze test in female mice. Brain Behav. 2014;4:51-9 pubmed publisher
Nag S, Mokha S. Activation of a Gq-coupled membrane estrogen receptor rapidly attenuates ?2-adrenoceptor-induced antinociception via an ERK I/II-dependent, non-genomic mechanism in the female rat. Neuroscience. 2014;267:122-34 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
Engelstoft M, Park W, Sakata I, Kristensen L, Husted A, Osborne Lawrence S, et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab. 2013;2:376-92 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
Chimento A, Casaburi I, Bartucci M, Patrizii M, Dattilo R, Avena P, et al. Selective GPER activation decreases proliferation and activates apoptosis in tumor Leydig cells. Cell Death Dis. 2013;4:e747 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
Chimento A, Sirianni R, Casaburi I, Ruggiero C, Maggiolini M, Ando S, et al. 17?-Estradiol activates GPER- and ESR1-dependent pathways inducing apoptosis in GC-2 cells, a mouse spermatocyte-derived cell line. Mol Cell Endocrinol. 2012;355:49-59 pubmed publisher
image
image 1 :
Tocris Bioscience 3577/10 image 1
Cat.No. 3577 - G-1 C21H18BrNO3 CAS No. 881639-98-1
product information
master code :
3577
SKU :
3577/10
product name :
G-1
unit size :
10 mg
description :
Potent and selective GPER agonist
target :
Estrogen and Related Receptor Agonists
category :
Small Molecules
purity :
98%
observed molecular weight :
412.28
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
G-1 is a potent and selective GPER agonist (Ki = 11 nM, EC50 = 2 nM); displays no activity at ER and ER at concentrations up to 10 M. Increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro . Blocks MCF-1 cell cycle progression at the G1 phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis. Also inhibits glutamate-induced autophagy and neuronal loss in cultured primary cortical neurons.
top caption :
Potent and selective GPER agonist
extended description :
Potent and selective GPER agonist
chemical name text :
( )-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone
formula :
C21H18BrNO3
formula text :
C21H18BrNO3
cas num :
881639-98-1
USD :
276 USD
product details :
Potent and selective GPER agonist
storage :
Store at -20░C
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