G15;G-15;G 15;1161002-05-6

生物活性靶点体外研究体内研究 G15;G-15;G 15;1161002-05-6 试剂级价格

CAS号:1161002-05-6
英文名:(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
中文名:G15;G-15;G 15;1161002-05-6
CBNumber:CB32518797
分子式:C19H16BrNO2
分子量:370.24
MOL File:1161002-05-6.mol

G15;G-15;G 15;1161002-05-6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 :Store at -20°C
溶解度 :insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO
形态 :solid
酸度系数(pKa) :3.98±0.40(Predicted)
颜色 :White to off-white

G15;G-15;G 15;1161002-05-6性质、用途与生产工艺

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
Target Value
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.