G-15
Catalog No.: GC16618Purity:>99.00%
G-15 هو مضاد لمستقبلات هرمون الاستروجين المقترن ببروتين G عالي التقارب وانتقائي (GPER / GPR30) مع Ki من 20 نانومتر.
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
Cas No.: 1161002-05-6
10mM (in 1mL DMSO)In Stock
$55.00
1
1mgIn Stock
$23.00
1
5mgIn Stock
$50.00
1
10mgIn Stock
$87.00
1
25mgIn Stock
$167.00
1
50mgIn Stock
$266.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $55.00 | In Stock | 1 | |
| 1mg | $23.00 | In Stock | 1 | |
| 5mg | $50.00 | In Stock | 1 | |
| 10mg | $87.00 | In Stock | 1 | |
| 25mg | $167.00 | In Stock | 1 | |
| 50mg | $266.00 | In Stock | 1 |
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المراجع (Citations)
2 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
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.
البروتوكول (Protocol)
| 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. | |
وثائق المنتج (Product Documents)
Purity:>99.00%Appearance:A solid
البيانات البيولوجية (Biological Data)
1 / 1
الخصائص الكيميائية (Chemical Properties)
رقم CAS
1161002-05-6
الاسم الكيميائي
(3aR,4R,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
SMILES
BrC1=C(C=C2OCOC2=C1)[C@@H]3NC4=CC=CC=C4[C@@H]5[C@H]3CC=C5
الصيغة الجزيئية
C19H16BrNO2
الوزن الجزيئي
370.24
الذوبانية
≥ 37mg/mL in DMSO
التخزين
-20°C, protect from light
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
g/mol
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