Name: G-15
Price: 292.00 USD

- Overview
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    Background
    
    G-15 is a selective antagonist of GPR30 with Ki value of 20 nM [1].
    G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].
    G-15 is a selective GPR30 antagonist with Ki value of 20 nM, While displayed little binding to ERα or ERβ up to 10 μM. In SKBr3 breast cancer cells that expressed only GPR30, G-1 or estrogen significantly increased intracellular calcium concentrations, while G15 inhibited the response to G-1 or estrogen with IC50 value of 185 and 190 nM respectively in a dose-dependent way. In GPR30-transfected COS7 cells, G-15 inhibited both estrogen and G-1 activation of PI3K and accumulation of PIP3 [1]. In endometriotic cells, G-1 increased cell proliferation and Akt phosphorylation, while G-15 reversed this stimulation and inhibited cell proliferation and induced Akt dephosphorylation [2].
    In intact rats and ovariectomized (OVX) rats treated with estradiol, G-15 impaired acquisition of delayed matching-to-position (DMP) T-maze task with a persistent turn. The result suggested that GPR30 played an crucial role in mediating the effects of estradiol on spatial learning [3].
    
    [1] Dennis MK, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist. Nat Chem Biol, 2009, 5 (6): 421-427.
    [2] G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells. Fertil Steril, 2013, 100 (3): 770-776.
    [3] Hammond R, Nelson D, Kline E, et al. Chronic treatment with a GPR30 antagonist impairs acquisition of a spatial learning task in young female rats. Horm Behav, 2012, 62 (4): 367-374.
- Properties
  - Categories
    
    GPER receptor antagonist
    
    Alternative Name
    
    (3aR,4S,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
    
    CAS Number
    
    1161002-05-6
    
    Molecular Formula
    
    C19H16BrNO2
    
    Molecular Weight
    
    370.24
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    BrC1=C([[email protected]]2NC3=CC=CC=C3[[email protected]]4([H])[[email protected]@]2([H])CC=C4)C=C5OCOC5=C1
    
    * For Research Use Only
- Reference
  - 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. 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
    3. 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
    4. 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
    5. Feiyan Meng, Lihong Zhang, et al. "Two forms of G protein-coupled estrogen receptor 1 in the ricefield eel: Expression and functional characterization in relation to ovarian follicle development." Gen Comp Endocrinol. 2021 Apr 1;304:113720. PMID:33508329
    6. Liping Gu, Yunyan Ke, et al. "Berberine suppresses bone loss and inflammation in ligature-induced periodontitis through promotion of the G protein-coupled estrogen receptor-mediated inactivation of the p38MAPK/NF-κB pathway." Archives of Oral Biology.Volume 122, February 2021, 104992. PMID:33338754
    7. Zhao B, Xiong Y, et al. "Rutin promotes osteogenic differentiation of periodontal ligament stem cells through the GPR30-mediated PI3K/AKT/mTOR signaling pathway." Exp Biol Med (Maywood). 2020;1535370220903463. PMID:32036685
    8. Yang S, Cheng W, et al. "Use of embryonic stem cell-derived cardiomyocytes to study cardiotoxicity of bisphenol AF via the GPER/CAM/eNOS pathway." Toxicology. 2020;432:152380. PMID:31981723
    9. Qing-changWua, Xi-yangTanga, et al. "Sweroside promotes osteoblastic differentiation and mineralization via interaction of membrane estrogen receptor-α and GPR30 mediated p38 signalling pathway on MC3T3-E1 cells." Phytomedicine. Available online 7 December 2019, 153146.
    10. 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
    11. 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
    12. 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

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

G-15

G-15

Background

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