G-36 is a cell permeable, nonsteroidal, high-affinity, selective antagonist of GPER. GPER/GPR30 is a seven-
transmembrane G protein-coupled estrogen receptor that regulates many aspects of mammalian biology and
physiology. G36 is available in addition to the previously described GPER-selective agonist G-1 (AZ00001-G36)
and antagonist G15 (AZ00001-G15), all based on a tetrahydro-3H-cyclopenta[c]quinoline scaffold. G36 shows
decreased binding and activation of ERa compared to G15, while maintaining its antagonist profile towards
GPER. G36 selectively inhibits estrogen-mediated activation of PI3K by GPER but not ERa. It also inhibits
estrogen- and G-1-mediated calcium mobilization as well as ERK1/2 activation, with no effect on EGF-
mediated ERK1/2 activation. Similar to G15, G36 inhibits estrogen- and G-1-stimulated proliferation of uterine
epithelial cells in vivo. The identification of G36 as a GPER antagonist with improved ER counterselectivity
represents a significant step towards the development of new highly selective therapeutics for cancer and
other diseases.
| Formal Name | 3H-Cyclopena[c]quinoline, 4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro- 8-(1-methylethyl)-, (3aR,4S,9bS)-rel- |
| CAS Number | 1392487-51-2 |
| Molecular Formula |
C22 H22 BrNO2 |
| Formula Weight | 412.32 |
| Formulation | A crystalline solid |
| Purity | ≥98% |
| Stability | 2 years |
| Storage | -20°C |
| Shipping | Room temperature in continental US; may vary elsewhere |
| Solubility | DMSO up 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 | Antagonist |
|---|
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