G-1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
G-1是一种有效的和选择性的GPR30激动剂,EC50值为2 nM[1]。
G蛋白偶联受体30(GPR30)是一种整合膜蛋白,位于内质网中,与雌二醇和醛固酮具有高亲和性。GPR30参与多种细胞内信号通路[1]。
G-1是一种有效的和选择性的GPR30激动剂。在表达GPR30的细胞中,G-1与荧光雌激素竞争结合,Ki值为11 nM。而在表达ERɑ和ERβ的细胞中,当其浓度高达1 μM时仍没有实质性的结合。在表达GPR30的COS7细胞中,G-1以剂量依赖的方式显著增加细胞内钙离子的浓度,EC50值为2 nM。在仅表达GPR30的SKBr3乳腺癌细胞中,G-1激活PI3K,导致PIP3的核积累[1]。
在双侧卵巢切除(OVX)的雌性Sprague-Dawley大鼠中,ISO(85 mg/kg,17天)给药后获得心衰模型。G-1(120 μg/kg,14天)减少心脏纤维化和脑内利钠肽的浓度,增加心脏收缩。G-1还增加β2-AR的表达,并使β1-AR的表达标准化[2]。
参考文献:
[1]. Bologa CG, Revankar CM, Young SM, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol, 2006, 2(4): 207-212.
[2]. Kang S, Liu Y, Sun D, et al. Chronic activation of the G protein-coupled receptor 30 with agonist G-1 attenuates heart failure. PLoS One, 2012, 7(10): e48185.
- 1. Guanyu Chen, Honghui Zeng, et al. "Activation of G protein coupled estrogen receptor prevents chemotherapy-induced intestinal mucositis by inhibiting the DNA damage in crypt cell in an extracellular signal-regulated kinase 1- and 2- dependent manner." Cell Death Dis. 2021 Oct 30;12(11):1034. PMID:34718327
- 2. Dan Huang, Xindong Wang, et al. "Bazi Bushen Capsule Alleviates Post-Menopausal Atherosclerosis via GPER1-Dependent Anti-Inflammatory and Anti-Apoptotic Effects." Front Pharmacol. 2021 Jun 25;12:658998. PMID:34248622
- 3. Lixia Zhou, Tenghua Yu, et al. "G Protein-Coupled Estrogen Receptor Agonist G-1 Inhibits Mantle Cell Lymphoma Growth in Preclinical Models." Front Oncol. 2021 Jun 15;11:668617. PMID:34211844
- 4. Peng Wang, Li-Na Jiang, et al. "Estradiol-induced inhibition of endoplasmic reticulum stress normalizes splenic CD4 + T lymphocytes following hemorrhagic shock." Sci Rep. 2021 Apr 5;11(1):7508. PMID:33820957
- 5. Xiaoyu Hang, Zhenyu Zhang, et al. "Estrogen Protects Articular Cartilage by Downregulating ASIC1a in Rheumatoid Arthritis." J Inflamm Res. 2021 Mar 12;14:843-858. PMID:33737825
- 6. Zhong J, Ge HF, et al. "G Protein-Coupled Estrogen Receptor 1 Negatively Regulates the Proliferation of Mouse-Derived Neural Stem/Progenitor Cells via Extracellular Signal-regulated Kinase Pathway." Brain Res. 2019 Feb 21. pii: S0006-8993(19)30108-8. PMID:30797747
- 7. Chang Y, Han Z, et al. "G protein-coupled estrogen receptor activation improves contractile and diastolic functions in rat renal interlobular artery to protect against renal ischemia reperfusion injury." Biomed Pharmacother. 2019 Apr;112:108666. PMID:30784936
- 8. Chai S, Liu K, et al. "Activation of G protein-coupled estrogen receptor protects intestine from ischemia/reperfusion injury in mice by protecting the crypt cell proliferation." Clin Sci (Lond). 2019 Feb 8;133(3):449-464. PMID:30705108
- 9. Wu Y, Feng D, et al. "Downregulation of G protein coupled receptor 30 in the hippocampus attenuates the neuroprotection of estrogen in the critical period hypothesis." Mol Med Rep. 2018 Apr;17(4):5716-5725. PMID:29484405
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 412.28 |
Cas No. | 881639-98-1 |
Formula | C21H18BrNO3 |
Solubility | ≥41.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one |
SDF | Download SDF |
Canonical SMILES | CC(C1=CC=C(C([C@@]2([H])[C@]3([H])CC=C2)=C1)N[C@H]3C4=C(Br)C=C(OCO5)C5=C4)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
SKBr3乳腺癌细胞和MCF7细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
10 nM |
实验结果 |
在仅表达GPR30的SKBr3细胞以及表达GPR30和ERα/β的MCF7细胞中,G-1促进PIP3于细胞核内积累。此外,G-1抑制SKBr3和MCF7细胞迁移,其IC50值分别为0.7 nM和1.6 nM。因此,在含ERs的细胞中,G-1可以选择性地结合GPR30,激活内源性表达的GPR30,诱发各种生理反应,如抑制细胞迁移。 |
动物实验 [2]: | |
动物模型 |
接受双侧卵巢切除术并伴有心衰的雌性Sprague-Dawley大鼠 |
给药剂量 |
120 μg/kg;持续14天 |
实验结果 |
在接受双侧卵巢切除术的并伴有心衰的雌性Sprague-Dawley大鼠中,G-1治疗降低了脑钠肽的浓度、抑制心脏纤维化并促进心脏收缩。G-1通过恢复β1-AR表达和上调β2-AR表达以持续激活GPR30,从而缓解心力衰竭。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Bologa CG, Revankar CM, Young SM, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol, 2006, 2(4): 207-212. [2]. Kang S, Liu Y, Sun D, et al. Chronic activation of the G protein-coupled receptor 30 with agonist G-1 attenuates heart failure. PLoS One, 2012, 7(10): e48185. |
质量控制和MSDS
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