881639-98-1
中文名称 | 881639-98-1 |
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中文同义词 | 化合物G-1;1-((3AR,4S,9BS)-REL-4-(6-溴苯并[D][1,3]二氧杂环己烷基-5-基)-3A,4,5,9B-四氢-3H-环戊烷[C]喹啉-8-基)乙酮;1-((3AR,4S,9BS)-REL-4-(6-溴苯并[D][1,3]二恶英-5-基)-3A,4,5,9B-四氢-3H-环戊烷[C]喹啉-8-基)乙酮;G-1,GPER激动剂 |
英文名称 | (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone |
英文同义词 | (±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone;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;G-06710-1;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-;1-((3aR,4S,9bS)-rel-4-(6-Bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethanone;G1,Inhibitor,G-1,inhibit,G 1,Estrogen Receptor/ERR |
CAS号 | 881639-98-1 |
分子式 | C21H18BrNO3 |
分子量 | 412.28 |
EINECS号 | |
相关类别 | |
Mol文件 | 881639-98-1.mol |
结构式 |
881639-98-1 性质
沸点 | 529.6±50.0 °C(Predicted) |
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密度 | 1.457±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMSO 中≥41.2 mg/mL;不溶于水;不溶于乙醇 |
形态 | 结晶固体 |
酸度系数(pKa) | 1.20±0.40(Predicted) |
颜色 | 白色至米白色 |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | S0851 | 881639-98-1 G-1 | 881639-98-1 | 1mg | 1270.46元 |
2024/08/19 | S0851 | 881639-98-1 G-1 | 881639-98-1 | 5mg | 2970元 |