G15 是一种高亲和力的、选择性的 G 蛋白偶联雌激素受体(GPER/GPR30)拮抗剂(Ki:20 nM)。

G15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM)

G-15 antagonizes the anti-depressive effects of estrogen in vivo[1].

G15 and G1 were first dissolved in DMSO and diluted with saline; the final concentration in DMSO was 1 mM. Desipramine and E2 (cyclodextrin-encapsulated, 4-5.5% E2) were dissolved in saline solution and DMSO was added to a final concentration of 1 mM. An appropriate vehicle-treated group (saline with 1 mM DMSO) was included as a control (sham). All solutions were freshly prepared before each experimental series. Independent groups of mice (n=12-16) were treated with two consecutive intraperitoneal injections as follows: vehicle solution + vehicle solution (sham group); vehicle + G-1 (indicated amount in nmol); vehicle + desipramine (10mg/kg); G15 (10nmol/mouse) + desipramine (10mg/kg); G15 (10nmol/mouse) + G-1 (1nmol/mouse); vehicle + G15 (10nmol/mouse); vehicle + soluble E2 (5 mg/kg); G15 (25nmol/mouse) + soluble E2 (5 mg/kg). The second compound was injected 15 min (7 min for E2) after the first injection and the tail suspension test performed 30 min after the second injection[1].

1161002-05-6

C19H16BrNO2

370.246

DMSO:41.67 mg/mL (112.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years