G15

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

G15 是 GPER 的细胞渗透性非类固醇拮抗剂 (Ki = 20 nM)。

G15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).

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.

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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Endocrinology/Hormones

Estrogen Receptor/ERR

GPER

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1161002-05-6

370.24

C19H16BrNO2

>98% (HPLC)

DMSO:41.67 mg/mL (112.55 mM)

[H][C@]12CC=C[C@@]1([H])c1ccccc1N[C@H]2c1cc2OCOc2cc1Br

(3aS4R9bR)-4-(6-bromo-13-benzodioxol-5-yl)-3a459b-tetrahydro-3H-cyclopenta[c]quinoline

(-20℃)

With Ice Pack

≥ 2 years