G15;G-15;G 15;1161002-05-6
| 中文名称 | G15;G-15;G 15;1161002-05-6 |
|---|---|
| 中文同义词 | (3AS,4R,9BR)-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;化合物G15;15国集团;ANTI-AGPAT1 ANTIBODY-溶血磷脂酰基转移酶抗体;G-15,GPER拮抗剂 |
| 英文名称 | (3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline |
| 英文同义词 | G-15;(3aS,4R,9bR)-4-(6-BroMo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline;H37;LUCA15;RMB5;RNA binding motif protein 5;1-AGPAT1;AGPAT1 |
| CAS号 | 1161002-05-6 |
| 分子式 | C19H16BrNO2 |
| 分子量 | 370.24 |
| EINECS号 | |
| 相关类别 | 试剂盒-细胞分析试剂盒;小分子 |
| Mol文件 | 1161002-05-6.mol |
| 结构式 |  |
G15;G-15;G 15;1161002-05-6 性质
| 熔点 | 178-180 °C |
|---|---|
| 沸点 | 462.7±45.0 °C(Predicted) |
| 密度 | 1.472±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 不溶于水；不溶于乙醇； DMSO 中≥37 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.98±0.40(Predicted) |
G15是一种高亲和力、选择性的G-protein coupled estrogen receptor 1 (GPER, GPR30) 拮抗剂，约20 nM的结合亲和力，在浓度高达10 μM时，对ERα和ERβ没有亲和力。
| Target | Value |
|
GPER
() |
G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines.
G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines.
Cell Proliferation Assay
| Cell Line: | A549, H1793 cell lines |
| Concentration: | 0.1, 1, 10 μM (combination with 10 nM E2) |
| Incubation Time: | 2 days |
| Result: | Inhibited GPER-mediated proliferation stimulated by E2. |
Western Blot Analysis
| Cell Line: | A549, H1793 cell lines |
| Concentration: | 1 μM (combination with 10 nM E2 and 10 nM G1) |
| Incubation Time: | 48 hours |
| Result: | Inhibited the response of GPER stimulated by E2 and G1. |
G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice.
| Animal Model: | Four-week-old female Kunming mice (Urethane-induced adenocarcinoma) |
| Dosage: | 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) |
| Administration: | Subcutaneous injection; twice a week for 14 weeks |
| Result: | The number of tumor nodules decreased in the E2+Ful+G15 group. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-103449 | G15;G-15;G 15;1161002-05-6 G15 | 1161002-05-6 | 5mg | 712元 |
| 2024/04/30 | HY-103449 | G15;G-15;G 15;1161002-05-6 G15 | 1161002-05-6 | 10mM * 1mLin DMSO | 783元 |