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1161002-05-6

中文名称 G15;G-15;G 15;1161002-05-6
英文名称 (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 结构式 1161002-05-6 结构式

基本信息

中文别名
15国集团
化合物G15
(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
英文别名
H37
G-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

物理化学性质

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-20°C储存
溶解度insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO
酸度系数(pKa)3.98±0.40(Predicted)
形态固体
G15;G-15;G 15;1161002-05-6价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-103449G15;G-15;G 15;1161002-05-6
G15
1161002-05-65mg712元
2024/04/30HY-103449G15;G-15;G 15;1161002-05-6
G15
1161002-05-610mM * 1mLin DMSO783元
2024/04/30HY-103449G15;G-15;G 15;1161002-05-6
G15
1161002-05-610mg1235元

常见问题列表

生物活性
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。
靶点
TargetValue
GPER
()
体外研究

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.
体内研究

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.
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