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  3. G15

G15 

目录号: HY-103449
产品使用指南

G15 是一种高亲和力和选择性 G 蛋白偶联雌激素受体 (GPER) 拮抗剂,Ki 值为 20 nM。

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G15 Chemical Structure

G15 Chemical Structure

CAS No. : 1161002-05-6

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Description

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER) antagonist with a Ki of 20 nM[1][2].

IC50 & Target

Ki: 20 nM (G-protein-coupled estrogen receptor)[2]

In Vitro

G15 (0.1-10 μM; 2 days) inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines[1].
G15 (1 μM; 48 hours) inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines[1].

Cell Proliferation Assay[1]

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[1]

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.
In Vivo

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[1].

Animal Model: Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1]
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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

370.24

Formula

C₁₉H₁₆BrNO₂

CAS No.

1161002-05-6

SMILES

BrC1=C([C@@H]2NC3=C(C=CC=C3)[C@@]4([H])[C@]2([H])CC=C4)C=C5OCOC5=C1

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
G15
目录号:
HY-103449
需求量:

G15

Cat. No.: HY-103449