G-1

• Supplier: Tocris Bioscience
• Catalog: 5446
• Prices: $189.00, $765.00
• Sizes: 10 mg, 50 mg
• Function Type: Agonist
• Cas Number: 881639-98-1
• Chemical 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
• Formula: C21H18BrNO3
• Molecular Weight: 412.28
• Purity: >98 %
• Description: Potent and selective GPER agonist (K i = 11 nM, EC 50 = 2 nM); displays no activity at ER α and ER β at concentrations up to 10 μ M. Increases cytosolic Ca 2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC 50 values are 0.7 and 1.6 nM respectively) in vitro . Blocks MCF-1 cell cycle progression at the G 1 phase. Displays therapeutic effects in the mouse EAE model of multiple sclerosis.

Product References

G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth - G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth

Albanito L, Madeo A, Lappano R, Vivacqua A, Rago V, Carpino A, Oprea TI, Prossnitz ER, Musti AM, Ando S, Maggiolini M. Cancer Res. 2007 Feb 15;67(4):1859-66.

Beneficial role of the GPR30 agonist G-1 in an animal model of multiple - Beneficial role of the GPR30 agonist G-1 in an animal model of multiple

Blasko E, Haskell CA, Leung S, Gualtieri G, Halks-Miller M, Mahmoudi M, Dennis MK, Prossnitz ER, Karpus WJ, Horuk R. J Neuroimmunol. 2009 Sep 29;214(1-2):67-77.

The G protein-coupled receptor GPR30 inhibits proliferation of estrogen - The G protein-coupled receptor GPR30 inhibits proliferation of estrogen

Ariazi EA, Brailoiu E, Yerrum S, Shupp HA, Slifker MJ, Cunliffe HE, Black MA, Donato AL, Arterburn JB, Oprea TI, Prossnitz ER, Dun NJ, Jordan VC. Cancer Res. 2010 Feb 1;70(3):1184-94.