Potent and selective GPER agonist
G-1 is a potent and selective 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. Also inhibits glutamate-induced autophagy and neuronal loss in cultured primary cortical neurons.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-151315 |
| Réf. fabricant | 18094882 |
| Nom chimique ou matériau | (±)-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 | 881639-98-1 |
| Quantité | 10 mg |
| Cible | Estrogen and Related Receptor Agonists |
| Formule moléculaire | C<sub>21</sub>H<sub>18</sub>BrNO<sub>3</sub> |
| Pureté | 98% |
