G-1 是一种高亲和力的、非甾体的、有选择性的GPR30激动剂(Ki:11 nM)。

G-1 is a nonsteroidal, high-affinity and selective GPR30 agonist (Ki: 11 nM).

Treatment with G-1 (10 μM and 100 μM; 48 and 72 h) obviously reduces cell proliferation (P<0.001). At 72 h, the IC50 value for G-1 is calculated to be 20 μM. Cell cycle analysis of H295R cells after 24 h of G-1 treatment shows a cell cycle arrest in the G2 phase. Treatment of A549 cells with G-1(20 μM) reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001)[2]. The presence of G-1 increases Bax expression while reduces Bcl-2[3].

After 14 days post-injury, the results display that the Basso mouse scale scores are obviously higher in the G-1 group compared with the other groups (P<0.05). G-1 administration produces a statistically significant induce in tumor volume from day 14 post-treatment. Grafted tumors harvested after a three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle-treated animals[3]. The number of caspase-3-positive cells in the cross-sections is counted, and G-1 group has fewer positive cells compared with the other groups (P<0.05), and there is no difference between the two groups (P>0.05)[1].

881639-98-1

C21H18BrNO3

412.28

DMSO:50 mg/mL (121.28 mM),Need ultrasonic
H2O:< 0.1 mg/mL (insoluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years