G15, GPER Antagonist

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G-15 is a cell permeable, nonsteroidal, high-affinity, selective antagonist of GPER that binds GPER with affinity of about 20-30 nM, 1/3 that of G-1 (AZ00001-G15)). G15 inhibits GPER-mediated calcium mobilization in human breast carcinoma SKBr3 cells (IC50 ~190 nM against stimulation by either 100 nM G-1 or 30 nM 17β-estradiol) in vitro and blocks G-1-induced (0.5 nmol per animal via s.c.) uterine epithelial proliferation (by ≥76% with ≥7.4 nmol G15 per animal via s.c.) in ovariectomized mice in vivo.

 

Sandia Biotech G15-Receptors

 
Formal Name (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
CAS Number 1161002-05-6
Molecular Formula

C19 H16 BrNO2

Formula Weight 370.2
Formulation A crystalline solid
Purity ≥97% by HPLC (Racemic mixture)
Stability 2 years
Storage -20°C
Shipping Room temperature
Solubility DMSO up to 50mM
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GPER Antagonist
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