G15

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G15  纯度: ≥99.0%

G15 是一种高亲和力和选择性 G 蛋白偶联雌激素受体 (GPER/GPR30) 拮抗剂，Ki 值为 20 nM。

G15

G15 Chemical Structure

CAS No. : 1161002-05-6

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10 mM * 1 mL in DMSO ￥935 In-stock
5 mg ￥850 In-stock
10 mg ￥1400 In-stock
50 mg ￥4300 In-stock
100 mg ￥7400 In-stock
200 mg   询价  
500 mg   询价  

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G15 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM[1][2].

IC50 & Target

Ki: 20 nM (GPER/GPR30)[2]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

370.24

Formula

C19H16BrNO2
CAS 号

1161002-05-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 41.67 mg/mL (112.55 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7010 mL 13.5048 mL 27.0095 mL
5 mM 0.5402 mL 2.7010 mL 5.4019 mL
10 mM 0.2701 mL 1.3505 mL 2.7010 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.62 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.62 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Liu C, et al. G-Protein-Coupled Estrogen Receptor Antagonist G15 Decreases Estrogen-Induced Development of Non-Small Cell Lung Cancer. Oncol Res. 2019 Feb 21;27(3):283-292

    [2]. Girgert R, et al. Estrogen Signaling in ERα-Negative Breast Cancer: ERβ and GPER. Front Endocrinol (Lausanne). 2019 Jan 9;9:781.

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