881639-98-1
基本信息
1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethanone
(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone
Ethanone, 1-[(3aR,4S,9bS)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-, rel-
物理化學(xué)性質(zhì)
報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)格 |
2024/11/08 | S0851 | 881639-98-1 G-1 | 881639-98-1 | 1mg | 1270.46元 |
2024/11/08 | S0851 | 881639-98-1 G-1 | 881639-98-1 | 5mg | 2970元 |
2024/11/08 | S0851 | G-1 | 881639-98-1 | 10mM (1mL in DMSO) | 3595.41元 |
常見(jiàn)問(wèn)題列表
Target | Value |
GPR30
(Cell-free assay) | 11 nM(Ki) |
G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a K i of 11 nM. Treatment with G-1 (10 μM and 100 μM) for 48 and 72 h significantly decreases cell proliferation (P<0.001). At 72 h, the IC 50 value for G-1 is calculated to be 20 μM. Treatment of A549 cells with G-1 at a concentration of 20 μM reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001). Cell cycle analysis of H295R cells after 24 h of G-1 treatment demonstrates a cell cycle arrest in the G 2 phase. The presence of G-1 increases Bax expression while decreases Bcl-2.
The results at 14 days post-injury show that the Basso mouse scale (BMS) scores are significantly higher in the G-1 group compared with the other groups (P<0.05). The number of caspase-3-positive cells in the cross sections is counted, and G-1 group has fewer positive cells compare with the other groups (P<0.05), and there is no difference between the two groups (P>0.05). G-1 administration produces a statistically significant decrease in tumor volume from day 14 post treatment. Grafted tumors harvested after three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle treated animals.