(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Struktur

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

Bezeichnung:(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

CAS-Nr881639-98-1

Englisch Name:(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

CBNumberCB32518964

SummenformelC21H18BrNO3

Molgewicht412.28

MOL-Datei881639-98-1.mol

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone physikalisch-chemischer Eigenschaften

Siedepunkt	529.6±50.0 °C(Predicted)
Dichte	1.457±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	≥41.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Aggregatzustand	crystalline solid
pka	1.20±0.40(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
GPR30 is a transmembrane G protein-coupled receptor (GPCR) localized to endoplasmic reticulum (ER) that binds estradiol with high affinity, activating multiple intracellular signaling pathways. G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a K_i value of 11 nM. Competitive binding studies in estrogen receptor α- (ERα-) and ERβ-expressing cells yielded K_i values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial binding of G-1 at 1 μM. The discovery of G-1, a compound that does not bind classical ERs, should facilitate further physiological experiments to define the role of GPR30 in vivo.
Verwenden
G-1 is a potent and selective G protein-coupled estrogen receptor (GPER) agonist (Ki = 11 nM, EC50 = 2 nM); displays no activity at ERα and ERβ at concentrations up to 10 μM. 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.
Definition
ChEBI: 1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone is a member of quinolines.
Lager
Store at -20°C
Einzelnachweise
[1]. bologa cg, revankar cm, young sm, et al. virtual and biomolecular screening converge on a selective agonist for gpr30. nat chem biol, 2006, 2(4): 207-212.
[2]. kang s, liu y, sun d, et al. chronic activation of the g protein-coupled receptor 30 with agonist g-1 attenuates heart failure. plos one, 2012, 7(10): e48185.

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

Gefahreninformationscode (GHS)

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Chemische Eigenschaften,Einsatz,Produktion Methoden

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Chemische Eigenschaften,Einsatz,Produktion Methoden

(±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Anbieter Lieferant Produzent Hersteller Vertrieb Händler.