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  3. G15

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

For research use only. We do not sell to patients.

CAS No. : 1161002-05-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 40 publication(s) in Google Scholar

Other Forms of G15:

Top Publications Citing Use of Products

40 Publications Citing Use of MCE G15

WB
Others
RT-PCR
Cell Imaging/Staining

    G15 purchased from MedChemExpress. Usage Cited in: Poult Sci. 2025 Dec 5;105(1):106210.  [Abstract]

    Effects of selective receptor agonists (PPT, DPN and G-1) treatment (3 h) on PGR expression, and antagonist (ICI and G15) treatment (3 h) on E2-upregulated PGR expression, in cultured pituitary cells from female chicks.

    G15 purchased from MedChemExpress. Usage Cited in: Pharm Biol. 2023 Dec;61(1):499-513.  [Abstract]

    TMYX enhanced the dilation function of coronary microvessels in vitro, but this effect was inhibited by G-15.

    G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372.  [Abstract]

    J774A.1 cells were pre-treated with DHEA (50 μM) in the presence or absence of the GPER inhibitor G15 (1 μM) for 1 h, then stimulated with LPS for 4 h. The TLR4, p-ERK/ERK, LC3, p62, p-mTOR, and p-AMPK protein expression levels were measured by western blotting and quantified by Image J software.

    G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372.  [Abstract]

    J774A.1 cells were pre-treated with G1 (1 μM) for 1 h, then stimulated with LPS for 4 h, and the indicated protein expression levels were measured by western blotting and quantified by Image J software.

    G15 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Apr 19;13(4):372.  [Abstract]

    J774A.1 cells were pre-treated with DHEA (50 μM) in the presence or absence of the GPER inhibitor G15 (1 μM) for 1 h, then stimulated with LPS for 4 h, PI-positive dead cells in 5 randomly selected fluorescence microscope images were counted by Image J software, scale bar = 200 μm.

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    Description

    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]

    Cellular Effect
    Cell Line Type Value Description References
    SK-BR-3 IC50
    185 nM
    Compound: G15
    Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of G1-mediated calcium mobilization
    Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of G1-mediated calcium mobilization
    [PMID: 19430488]
    SK-BR-3 IC50
    190 nM
    Compound: G15
    Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of E2-mediated calcium mobilization
    Antagonist activity at GPR30 in human SKBr3 cells assessed as inhibition of E2-mediated calcium mobilization
    [PMID: 19430488]
    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].

    MedChemExpress (MCE) 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.
    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].

    MedChemExpress (MCE) 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
    Molecular Weight

    370.24

    Formula

    C19H16BrNO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    BrC1=C([C@@H]2NC3=C(C=CC=C3)[C@@]4([H])[C@]2([H])CC=C4)C=C5OCOC5=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 41.67 mg/mL (112.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.0%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7010 mL 13.5048 mL 27.0095 mL 67.5238 mL
    5 mM 0.5402 mL 2.7010 mL 5.4019 mL 13.5048 mL
    10 mM 0.2701 mL 1.3505 mL 2.7010 mL 6.7524 mL
    15 mM 0.1801 mL 0.9003 mL 1.8006 mL 4.5016 mL
    20 mM 0.1350 mL 0.6752 mL 1.3505 mL 3.3762 mL
    25 mM 0.1080 mL 0.5402 mL 1.0804 mL 2.7010 mL
    30 mM 0.0900 mL 0.4502 mL 0.9003 mL 2.2508 mL
    40 mM 0.0675 mL 0.3376 mL 0.6752 mL 1.6881 mL
    50 mM 0.0540 mL 0.2701 mL 0.5402 mL 1.3505 mL
    60 mM 0.0450 mL 0.2251 mL 0.4502 mL 1.1254 mL
    80 mM 0.0338 mL 0.1688 mL 0.3376 mL 0.8440 mL
    100 mM 0.0270 mL 0.1350 mL 0.2701 mL 0.6752 mL
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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    G15
    Cat. No.:
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