Home Other Building Blocks GPR30 Agonist, G-1

GPR30 Agonist, G-1

CAS No.:
881639-98-1
Catalog Number:
AG008C1B
Molecular Formula:
C21H18BrNO3
Molecular Weight:
412.2765
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
1mg
99%
1 week
United States
$126
- +
5mg
99%
1 week
United States
$187
- +
10mg
99%
1 week
United States
$265
- +
50mg
99%
1 week
United States
$682
- +
100mg
99%
1 week
United States
$960
- +
Product Description
Catalog Number:
AG008C1B
Chemical Name:
GPR30 Agonist, G-1
CAS Number:
881639-98-1
Molecular Formula:
C21H18BrNO3
Molecular Weight:
412.2765
MDL Number:
MFCD16618392
IUPAC Name:
1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone
InChI:
InChI=1S/C21H18BrNO3/c1-11(24)12-5-6-18-15(7-12)13-3-2-4-14(13)21(23-18)16-8-19-20(9-17(16)22)26-10-25-19/h2-3,5-9,13-14,21,23H,4,10H2,1H3
InChI Key:
VHSVKVWHYFBIFJ-UHFFFAOYSA-N
SMILES:
CC(=O)c1ccc2c(c1)C1C=CCC1C(N2)c1cc2OCOc2cc1Br
Properties
Complexity:
596  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
411.047g/mol
Formal Charge:
0
Heavy Atom Count:
26  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
1  
Isotope Atom Count:
0
Molecular Weight:
412.283g/mol
Monoisotopic Mass:
411.047g/mol
Rotatable Bond Count:
2  
Topological Polar Surface Area:
47.6A^2
Undefined Atom Stereocenter Count:
3  
Undefined Bond Stereocenter Count:
0
XLogP3:
4.6  
Literature
Title Journal
The G protein-coupled oestrogen receptor 1 agonist G-1 disrupts endothelial cell microtubule structure in a receptor-independent manner. Molecular and cellular biochemistry 20120701
Effects of a combined treatment with GPR30 agonist G-1 and herceptin on growth and gene expression of human breast cancer cell lines. Cancer investigation 20120601
Activation of GPR30 attenuates diastolic dysfunction and left ventricle remodelling in oophorectomized mRen2.Lewis rats. Cardiovascular research 20120401
Aberrant ligand-induced activation of G protein-coupled estrogen receptor 1 (GPER) results in developmental malformations during vertebrate embryogenesis. Toxicological sciences : an official journal of the Society of Toxicology 20120101
G protein-coupled estrogen receptor 1-mediated effects in the rat myometrium. American journal of physiology. Cell physiology 20111101
Estrogen receptor GPR30 reduces oxidative stress and proteinuria in the salt-sensitive female mRen2.Lewis rat. Hypertension (Dallas, Tex. : 1979) 20111001
Induction of interleukin-10 in the T helper type 17 effector population by the G protein coupled estrogen receptor (GPER) agonist G-1. Immunology 20110901
Mechanisms of estradiol-induced insulin secretion by the G protein-coupled estrogen receptor GPR30/GPER in pancreatic beta-cells. Endocrinology 20110801
Insulinotropic and antidiabetic effects of 17β-estradiol and the GPR30 agonist G-1 on human pancreatic islets. Endocrinology 20110701
Estrogen destabilizes microtubules through an ion-conductivity-independent TRPV1 pathway. Journal of neurochemistry 20110601
Vasodilation in response to the GPR30 agonist G-1 is not different from estradiol in the mRen2.Lewis female rat. Journal of cardiovascular pharmacology 20110501
GPR30 activation opposes estrogen-dependent uterine growth via inhibition of stromal ERK1/2 and estrogen receptor alpha (ERα) phosphorylation signals. Endocrinology 20110401
GPR30 co-localizes with cholinergic neurons in the basal forebrain and enhances potassium-stimulated acetylcholine release in the hippocampus. Psychoneuroendocrinology 20110201
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 of vascular research 20110101
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. Cell death and differentiation 20100901
Signaling via GPR30 protects the myocardium from ischemia/reperfusion injury. Surgery 20100801
Expression and signaling of G protein-coupled estrogen receptor 1 (GPER) in rat sertoli cells. Biology of reproduction 20100801
Dilation of epicardial coronary arteries by the G protein-coupled estrogen receptor agonists G-1 and ICI 182,780. Pharmacology 20100801
Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs. Organic & biomolecular chemistry 20100507
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. Molecular endocrinology (Baltimore, Md.) 20100501
Endothelium-dependent relaxation by G protein-coupled receptor 30 agonists in rat carotid arteries. American journal of physiology. Heart and circulatory physiology 20100301
The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells. Cancer research 20100201
Attenuation of salt-induced cardiac remodeling and diastolic dysfunction by the GPER agonist G-1 in female mRen2.Lewis rats. PloS one 20100101
Activation of a novel estrogen receptor, GPER, is cardioprotective in male and female rats. American journal of physiology. Heart and circulatory physiology 20091101
Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. Journal of neuroimmunology 20090929
Chronic treatment with estrogen receptor agonists restores acquisition of a spatial learning task in young ovariectomized rats. Hormones and behavior 20090901
Chronic treatment with the G protein-coupled receptor 30 agonist G-1 decreases blood pressure in ovariectomized mRen2.Lewis rats. Endocrinology 20090801
Expression of estrogen receptor GPR30 in the rat spinal cord and in autonomic and sensory ganglia. Journal of neuroscience research 20090515
Involvement of estradiol-17beta and its membrane receptor, G protein coupled receptor 30 (GPR30) in regulation of oocyte maturation in zebrafish, Danio rario. General and comparative endocrinology 20090301
Membrane estrogen receptor regulates experimental autoimmune encephalomyelitis through up-regulation of programmed death 1. Journal of immunology (Baltimore, Md. : 1950) 20090301
GPR30 estrogen receptor agonists induce mechanical hyperalgesia in the rat. The European journal of neuroscience 20080401
GPR30 contributes to estrogen-induced thymic atrophy. Molecular endocrinology (Baltimore, Md.) 20080301
Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system. The Journal of endocrinology 20070501
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. Cancer research 20070215
Microsphere-based protease assays and screening application for lethal factor and factor Xa. Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501
Properties