1161002-05-6
中文名稱
G15;G-15;G 15;1161002-05-6
英文名稱
(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
CAS
1161002-05-6
分子式
C19H16BrNO2
分子量
370.24
MOL 文件
1161002-05-6.mol
更新日期
2023/03/20 15:41:25
1161002-05-6 結(jié)構(gòu)式
基本信息
中文別名
15國(guó)集團(tuán)化合物G15
(3AS,4R,9BR)-4-(6-溴苯并[D][1,3]二惡英-5-基)-3A,4,5,9B-四氫-3H-環(huán)戊烷[C]喹啉
英文別名
H37G-15
RMB5
LUCA15
AGPAT1
1-AGPAT1
LPAAT-alpha
G15
G-15
G 15
1161002-05-6
RNA binding motif protein 5
Compound G15 - GPR30 antagonist
物理化學(xué)性質(zhì)
熔點(diǎn)178-180 °C
沸點(diǎn)462.7±45.0 °C(Predicted)
密度1.472±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO
酸度系數(shù)(pKa)3.98±0.40(Predicted)
形態(tài)固體
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
G15是一種高親和力、選擇性的G-protein coupled estrogen receptor 1 (GPER, GPR30) 拮抗劑，約20 nM的結(jié)合親和力，在濃度高達(dá)10 μM時(shí)，對(duì)ERα和ERβ沒(méi)有親和力。靶點(diǎn)
| Target | Value |
|
GPER
() |
體外研究
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. |
體內(nèi)研究
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. |