G-15
目录号 : GC16618
G-15是一种高亲和力、选择性的G蛋白偶联雌激素受体（GPER/ GPR30）拮抗剂（Ki = 20nM） 。
Cas No.:1161002-05-6
Sample solution is provided at 25 µL, 10mM.
G-15 is a high-affinity, selective antagonist of G protein-coupled estrogen receptor (GPER/ GPR30) (Ki = 20nM) [1]. G‑15 competes with GPER for ligand binding sites, thereby blocking the action of hormones on the receptor, thereby inhibiting cell growth, proliferation or migration [2]. G‑15 is commonly used in cancer treatment research [3-4].
In SCC4, SCC9, and HSC-3 cells, after G-15 (5-20μM; 24h. 48h) treatment, all three cell lines showed dose-dependent inhibition of cell proliferation [5]. In MCF-7, MDA-MB-231, Bcap-37 cells, higher concentrations of G15 (1.25µM, 2.5µM, 5.0µM; 48h) significantly inhibited the viability of these three cell lines [6]. In A549 cells, G-15 (1μM; 24h) treatment inhibited cell growth [7].
In C57BL/6 mice, G-15 (50μg/kg; sc; 6d) treatment decreased expression of GPER in all treated age groups, with a significant decrease in mature animals [8]. In C57BL/6 mice, G-15 (10μg/kg, 50μg/kg; sc; 10d) treatment antagonizes the increase in striatal HVA/DA ratio induced by G1 [9].
References:
[1]. Kang W B, Cong Y, Ru J Y, et al. Osteoprotective effect of combination therapy of low-dose oestradiol with G15, a specific antagonist of GPR30/GPER in ovariectomy-induced osteoporotic rats[J]. Bioscience reports, 2015, 35(4): e00239.
[2]. Xu F, Ma J, Wang X, et al. The role of G protein-coupled estrogen receptor (GPER) in vascular pathology and physiology[J]. Biomolecules, 2023, 13(9): 1410.
[3]. Zhu Z, Nie X, Deng L, et al. Regulation of cervical cancer via G15-mediated inhibition of G protein-coupled estrogen receptor[J]. Anti-Cancer Drugs, 2024, 35(9): 817-829.
[4]. Liu C, Liao Y, Fan S, et al. G-protein-coupled estrogen receptor antagonist G15 decreases estrogen-induced development of non-small cell lung cancer[J]. Oncology Research, 2019, 27(3): 283.
[5]. Bai L Y, Weng J R, Hu J L, et al. G15, a GPR30 antagonist, induces apoptosis and autophagy in human oral squamous carcinoma cells[J]. Chemico-biological interactions, 2013, 206(2): 375-384.
[6]. Liu Y, Du F Y, Chen W, et al. G15 sensitizes epithelial breast cancer cells to doxorubicin by preventing epithelial-mesenchymal transition through inhibition of GPR30[J]. American Journal of Translational Research, 2015, 7(5): 967.
[7]. Shen Y, Li C, Zhou L, et al. G protein‐coupled oestrogen receptor promotes cell growth of non‐small cell lung cancer cells via YAP1/QKI/circNOTCH1/m6A methylated NOTCH1 signalling[J]. Journal of cellular and molecular medicine, 2021, 25(1): 284-296.
[8]. Kotula-Balak M, Pawlicki P, Milon A, et al. The role of G-protein-coupled membrane estrogen receptor in mouse Leydig cell function—in vivo and in vitro evaluation[J]. Cell and Tissue Research, 2018, 374(2): 389-412.
[9]. Bourque M, Morissette M, Côté M, et al. Implication of GPER1 in neuroprotection in a mouse model of Parkinson's disease[J]. Neurobiology of aging, 2013, 34(3): 887-901.
G-15是一种高亲和力、选择性的G蛋白偶联雌激素受体（GPER/ GPR30）拮抗剂（Ki = 20nM） [1]。G-15与GPER竞争配体结合位点，从而阻断激素对受体的作用，进而抑制细胞生长、增殖或迁移 [2]。G-15常用于癌症治疗研究 [3-4]。
在SCC4、SCC9和HSC-3细胞中，经G-15（5-20μM；24h，48h）处理后，这三种细胞系均表现出剂量依赖性的细胞增殖抑制 [5]。在 MCF-7、MDA-MB-231和Bcap-37细胞中，较高浓度的G15（1.25µM，2.5µM，5.0µM；48h）显著抑制了这三种细胞系的活力 [6]。在A549细胞中，G-15（1μM；24h）处理可抑制细胞生长 [7]。
在C57BL/6小鼠中，G-15（50μg/kg；sc；6d）处理降低了所有治疗年龄组的GPER表达，且在成熟小鼠中显著降低 [8]。在C57BL/6小鼠中，G-15（10μg/kg，50μg/kg；sc；10d）处理可拮抗G1诱导的纹状体HVA/DA比率的升高 [9]。
| Cell experiment [1]: | |
Cell lines | SCC4, SCC9, and HSC-3 cells |
Preparation Method | SCC4, SCC9, and HSC-3 cells were seeded at 5 × 103 cells per well in 96-well flat-bottomed plates; then, 24h later, cells were treated with G15 or DMSO at the concentrations indicated in the individual figures. At the end of the treatment, the medium was removed, replaced by 200 lL DMEM/F12 containing 0.5mg/mL of MTT and cells were incubated in the CO2 incubator at 37℃ for 2h. Supernatants were aspirated from the wells, and the reduced MTT dye was solubilized in 200μL/well DMSO. |
Reaction Conditions | 5-20μM; 24h, 48h |
Applications | After G-15 treatment, all three cell lines showed dose-dependent inhibition of cell proliferation. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice from various age groups were allotted into experimental groups (each group including 5 animals); and control (Cont.) and treated receiving selective GPER receptor antagonist (G-15). G-15 was dissolved in DMSO and the stock solutions were kept at -20℃. Animals from the experimental groups were injected subcutaneously with freshly prepared solutions of G-15 (50μg/kg) in phosphate buffered saline. Mice from control groups received vehicle only. |
Dosage form | 50μg/kg; sc; 6d |
Applications | G-15 treatment decreased expression of GPER in all treated age groups, with a significant decrease in mature animals. |
[1]. Bai L Y, Weng J R, Hu J L, et al. G15, a GPR30 antagonist, induces apoptosis and autophagy in human oral squamous carcinoma cells[J]. Chemico-biological interactions, 2013, 206(2): 375-384. | |
| Cas No. | 1161002-05-6 | SDF | |
| 化学名 | (3aR,4R,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | ||
| Canonical SMILES | BrC1=C(C=C2OCOC2=C1)[C@@H]3NC4=CC=CC=C4[C@@H]5[C@H]3CC=C5 | ||
| 分子式 | C19H16BrNO2 | 分子量 | 370.24 |
| 溶解度 | ≥ 37mg/mL in DMSO | 储存条件 | -20°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.701 mL | 13.5048 mL | 27.0095 mL |
| 5 mM | 0.5402 mL | 2.701 mL | 5.4019 mL |
| 10 mM | 0.2701 mL | 1.3505 mL | 2.701 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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