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G-1 is a potent and selective agonist of GPR30 with EC50 value of 2 nM [1].

G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].

G-1 is a potent and selective GPR30 agonist. In GPR30-expressing cells, G-1 competed binding of the fluorescent estrogen with Ki value of 11 nM, while no substantial binding at concentrations up to 1 μM in ERɑ- and ERβ-expressing cells. In GPR30-expressing COS7 cells, G-1 significantly increased intracellular calcium concentrations with EC50 value of 2 nM in a dose-dependent way. In SKBr3 breast cancer cells that expressed only GPR30, G-1 activated PI3K and resulted in the nuclear accumulation of PIP3 [1].

In female Sprague–Dawley rats with bilateral ovariectomy (OVX), ISO (85 mg/kg for 17 days) was given to make the heart failure models. G-1 (120 μg/kg for 14 days) treatment reduced cardiac fibrosis and concentration of brain natriuretic peptide and increased contraction of the heart. Also, G-1 increased the expression of β2-AR and normalized the expression of β1-AR [2].

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