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881639-98-1,MFCD16618392
Catalog No.:AA008BYJ

881639-98-1 | GPR30 Agonist, G-1

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1mg
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5mg
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10mg
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25mg
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50mg
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  • Technical Information
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA008BYJ
Chemical Name:
GPR30 Agonist, G-1
CAS Number:
881639-98-1
Molecular Formula:
C21H18BrNO3
Molecular Weight:
412.2765
MDL Number:
MFCD16618392
SMILES:
CC(=O)c1ccc2c(c1)C1C=CCC1C(N2)c1cc2OCOc2cc1Br
Properties
Computed Properties
 
Complexity:
596  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
26  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
2  
Undefined Atom Stereocenter Count:
3  
XLogP3:
4.6  

Literature

Title: The G protein-coupled oestrogen receptor 1 agonist G-1 disrupts endothelial cell microtubule structure in a receptor-independent manner.

Journal: Molecular and cellular biochemistry 20120701

Title: Effects of a combined treatment with GPR30 agonist G-1 and herceptin on growth and gene expression of human breast cancer cell lines.

Journal: Cancer investigation 20120601

Title: Activation of GPR30 attenuates diastolic dysfunction and left ventricle remodelling in oophorectomized mRen2.Lewis rats.

Journal: Cardiovascular research 20120401

Title: Aberrant ligand-induced activation of G protein-coupled estrogen receptor 1 (GPER) results in developmental malformations during vertebrate embryogenesis.

Journal: Toxicological sciences : an official journal of the Society of Toxicology 20120101

Title: G protein-coupled estrogen receptor 1-mediated effects in the rat myometrium.

Journal: American journal of physiology. Cell physiology 20111101

Title: Estrogen receptor GPR30 reduces oxidative stress and proteinuria in the salt-sensitive female mRen2.Lewis rat.

Journal: Hypertension (Dallas, Tex. : 1979) 20111001

Title: Induction of interleukin-10 in the T helper type 17 effector population by the G protein coupled estrogen receptor (GPER) agonist G-1.

Journal: Immunology 20110901

Title: Mechanisms of estradiol-induced insulin secretion by the G protein-coupled estrogen receptor GPR30/GPER in pancreatic beta-cells.

Journal: Endocrinology 20110801

Title: Insulinotropic and antidiabetic effects of 17β-estradiol and the GPR30 agonist G-1 on human pancreatic islets.

Journal: Endocrinology 20110701

Title: Estrogen destabilizes microtubules through an ion-conductivity-independent TRPV1 pathway.

Journal: Journal of neurochemistry 20110601

Title: Vasodilation in response to the GPR30 agonist G-1 is not different from estradiol in the mRen2.Lewis female rat.

Journal: Journal of cardiovascular pharmacology 20110501

Title: GPR30 activation opposes estrogen-dependent uterine growth via inhibition of stromal ERK1/2 and estrogen receptor alpha (ERα) phosphorylation signals.

Journal: Endocrinology 20110401

Title: GPR30 co-localizes with cholinergic neurons in the basal forebrain and enhances potassium-stimulated acetylcholine release in the hippocampus.

Journal: Psychoneuroendocrinology 20110201

Title: The GPER1 agonist G-1 attenuates endothelial cell proliferation by inhibiting DNA synthesis and accumulating cells in the S and G2 phases of the cell cycle.

Journal: Journal of vascular research 20110101

Title: Activation of GPR30 inhibits the growth of prostate cancer cells through sustained activation of Erk1/2, c-jun/c-fos-dependent upregulation of p21, and induction of G(2) cell-cycle arrest.

Journal: Cell death and differentiation 20100901

Title: Signaling via GPR30 protects the myocardium from ischemia/reperfusion injury.

Journal: Surgery 20100801

Title: Expression and signaling of G protein-coupled estrogen receptor 1 (GPER) in rat sertoli cells.

Journal: Biology of reproduction 20100801

Title: Dilation of epicardial coronary arteries by the G protein-coupled estrogen receptor agonists G-1 and ICI 182,780.

Journal: Pharmacology 20100801

Title: Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs.

Journal: Organic & biomolecular chemistry 20100507

Title: Regulation of ERRalpha gene expression by estrogen receptor agonists and antagonists in SKBR3 breast cancer cells: differential molecular mechanisms mediated by g protein-coupled receptor GPR30/GPER-1.

Journal: Molecular endocrinology (Baltimore, Md.) 20100501

Title: Endothelium-dependent relaxation by G protein-coupled receptor 30 agonists in rat carotid arteries.

Journal: American journal of physiology. Heart and circulatory physiology 20100301

Title: The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.

Journal: Cancer research 20100201

Title: Attenuation of salt-induced cardiac remodeling and diastolic dysfunction by the GPER agonist G-1 in female mRen2.Lewis rats.

Journal: PloS one 20100101

Title: Activation of a novel estrogen receptor, GPER, is cardioprotective in male and female rats.

Journal: American journal of physiology. Heart and circulatory physiology 20091101

Title: Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis.

Journal: Journal of neuroimmunology 20090929

Title: Chronic treatment with estrogen receptor agonists restores acquisition of a spatial learning task in young ovariectomized rats.

Journal: Hormones and behavior 20090901

Title: Chronic treatment with the G protein-coupled receptor 30 agonist G-1 decreases blood pressure in ovariectomized mRen2.Lewis rats.

Journal: Endocrinology 20090801

Title: Expression of estrogen receptor GPR30 in the rat spinal cord and in autonomic and sensory ganglia.

Journal: Journal of neuroscience research 20090515

Title: Involvement of estradiol-17beta and its membrane receptor, G protein coupled receptor 30 (GPR30) in regulation of oocyte maturation in zebrafish, Danio rario.

Journal: General and comparative endocrinology 20090301

Title: Membrane estrogen receptor regulates experimental autoimmune encephalomyelitis through up-regulation of programmed death 1.

Journal: Journal of immunology (Baltimore, Md. : 1950) 20090301

Title: GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat.

Journal: The European journal of neuroscience 20080401

Title: GPR30 contributes to estrogen-induced thymic atrophy.

Journal: Molecular endocrinology (Baltimore, Md.) 20080301

Title: Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system.

Journal: The Journal of endocrinology 20070501

Title: G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells.

Journal: Cancer research 20070215

Title: Microsphere-based protease assays and screening application for lethal factor and factor Xa.

Journal: Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501

Title: Cheng Q, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice. Biosci Rep. 2016 Aug 31;36(4). pii: e00373.

Title: Kurt AH, et al. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells. Oncol Lett. 2015 Nov;10(5):3177-3182.

Title: Chimento A, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015 Aug 7;6(22):19190-203.

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