G-1 is a cell permeable, nonsteroidal, dihydroquinoline, high-affinity, selective agonist for GPER/GPR30, the transmembrane G protein-coupled estrogen receptor. G-1 competes for estrogen-binding to GPER with a Ki value of 11 nM. Competitive binding studies in ERα- and ERβ-expressing cells show little binding of G-1 up to 10 µM. The discovery of G-1, a compound that does not bind classical ERs, has greatly facilitated physiological experiments to define the role of GPER in vivo.
Formal Name | (±)-1-[(3aR*, 4S*, 9bS*)-4-(6-Bromo-1, 3-benzodioxol-5-yl)-3a, 4, 5, 9b-tetrahydro-3H-cyclopenta[c]quinoline-8-yl]-ethanone |
CAS Number | 881639-98-1 |
Molecular Formula |
C21 H18 BrNO3 |
Formula Weight | 412.3 |
Formulation | A crystalline solid |
Purity | ≥98% |
Stability | 2 years |
Storage | -20°C |
Shipping | Room temperature in continental US; may vary elsewhere |
Solubility | DMSO to 100mM |
Our products are intended for research use only and are not to be used for any other purpose, which includes but is not
limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of
consumption or application to humans or animals
GPER | Agonist |
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