2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. G-1

G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.

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

CAS No. : 881639-98-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of G-1:

G-1 Related Antibodies

Top Publications Citing Use of Products

28 Publications Citing Use of MCE G-1

In Vivo Efficacy Study
Cell Proliferation/Viability Assay
Bio/Physico-chemical Assay
Cell Imaging/Staining
WB

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2025 Sep 5.  [Abstract]

    Mean time of immobility during the FST after a single dose injection of vehicle (n = 45), ketamine (n = 14), ERα agonist PPT (n = 12), ERβ agonist DPN (n = 15), or GPR30 agonist G-1 (200 μg/mL, sc, single dose) (n = 12).

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Feb 21;30(1):28.  [Abstract]

    The proliferation of A549 and H1299 cells (as stated earlier) treated with G1 and H2O2 was determined using the plate cloning formation assay.

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Feb 21;30(1):28.  [Abstract]

    Cell viability was determined using the CCK8 assay after 48 h of G1 (1 μM) and H2O2 treatments in A549 and H1299 cells.

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Feb 21;30(1):28.  [Abstract]

    MDA levels in A549 and H1299 cells after treatment with G1 (1 μM), H2O2, or both for 48 h.

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Feb 21;30(1):28.  [Abstract]

    Representative phase-contrast images and viability staining (green indicates live cells, and red indicates dead cells) of A549 and H1299 cells treated with G1 (1 μM), RSL3, or Erastin.

    G-1 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Feb 21;30(1):28.  [Abstract]

    The activation of PI3K/AKT/mTOR signaling (the protein levels of p-PI3K, p-AKT, and p-mTOR) in A549 and H1299 cells treated with G1 for 24 and 48 h.

    View All Estrogen Receptor/ERR Isoform Specific Products:

    View All Isoforms
    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.

    IC50 & Target

    Ki: 11 nM (GPR30)[1]
    Cellular Effect
    Cell Line Type Value Description References
    COS-7 EC50
    2 nM
    Compound: 1, G-1
    Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry
    Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry
    		[PMID: 16520733]
    MCF7 IC50
    1.6 nM
    Compound: 1, G-1
    Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay
    Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay
    		[PMID: 16520733]
    SK-BR-3 IC50
    0.7 nM
    Compound: 1, G-1
    Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay
    Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay
    		[PMID: 16520733]
    In Vitro

    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM[1].
    Treatment with G-1 (10 μM and 100 μM) for 48 and 72 h significantly decreases cell proliferation (P<0.001). At 72 h, the IC50 value for G-1 is calculated to be 20 μM. Treatment of A549 cells with G-1 at a concentration of 20 μM reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001)[2].
    Cell cycle analysis of H295R cells after 24 h of G-1 treatment demonstrates a cell cycle arrest in the G2 phase. The presence of G-1 increases Bax expression while decreases Bcl-2[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    G-1 Related Antibodies
    In Vivo

    The results at 14 days post-injury show that the Basso mouse scale (BMS) scores are significantly higher in the G-1 group compared with the other groups (P<0.05). The number of caspase-3-positive cells in the cross sections is counted, and G-1 group has fewer positive cells compare with the other groups (P<0.05), and there is no difference between the two groups (P>0.05)[1].
    G-1 administration produces a statistically significant decrease in tumor volume from day 14 post treatment. Grafted tumors harvested after three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle treated animals[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    412.28

    Formula

    C21H18BrNO3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    BrC1=C([C@H]2[C@]3([H])[C@](C=CC3)([H])C4=CC(C(C)=O)=CC=C4N2)C=C5C(OCO5)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (121.28 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 2.4255 mL 12.1277 mL 24.2554 mL
    5 mM 0.4851 mL 2.4255 mL 4.8511 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. 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (6.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.06 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (12.13 mM); Suspended solution; Need ultrasonic

    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).
    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: 99.76%

    SDS (622 KB)

    COA (254 KB) HNMR (133 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    A549 human lung cancer cells are treated with various concentrations (10 nM, 100 nM, 1 μM, 10 μM and 100 μM) of G-1 in 96-well plates and incubated for 48 or 72 h. Following incubation, MTT solution is added to each well at a concentration of 0.5 mg/mL, and incubated for 4 h at 37°C. At the end of this period, 100 µL DMSO solvent is added to each well. The absorbance values [optical density (OD)] at 570 nm of the solution in each well are read using a spectrophotometer[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Four-week-old nu/nu-Forkhead box N1nu female mice are used in this study. H295R cells, 6×106, suspended in 100 μL PBS, are combined with 30 μL of Matrigel (4 mg/mL) and injected subcutaneously in the shoulder of each animal. Mice are treated 21 days after cell injection, when tumors have reached an average volume of about 200 mm3. Animals are randomly assigned to be treated with vehicle or G-1 at a concentration of 2 mg/kg/daily. Drug tolerability is assessed in tumor-bearing mice in terms of: a) lethal toxicity, i.e. any death in treated mice occurring before any death in control mice; b) body weight loss percentage=100-[(body weight on day x/body weight on day 1)×100], where x represents a day during the treatment period. Animals are sacrificed by cervical dislocation 42 days after cell injection[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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. 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 2.4255 mL 12.1277 mL 24.2554 mL 60.6384 mL
    5 mM 0.4851 mL 2.4255 mL 4.8511 mL 12.1277 mL
    10 mM 0.2426 mL 1.2128 mL 2.4255 mL 6.0638 mL
    15 mM 0.1617 mL 0.8085 mL 1.6170 mL 4.0426 mL
    20 mM 0.1213 mL 0.6064 mL 1.2128 mL 3.0319 mL
    25 mM 0.0970 mL 0.4851 mL 0.9702 mL 2.4255 mL
    30 mM 0.0809 mL 0.4043 mL 0.8085 mL 2.0213 mL
    40 mM 0.0606 mL 0.3032 mL 0.6064 mL 1.5160 mL
    50 mM 0.0485 mL 0.2426 mL 0.4851 mL 1.2128 mL
    60 mM 0.0404 mL 0.2021 mL 0.4043 mL 1.0106 mL
    80 mM 0.0303 mL 0.1516 mL 0.3032 mL 0.7580 mL
    100 mM 0.0243 mL 0.1213 mL 0.2426 mL 0.6064 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    G-1 Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    G-1881639-98-1G1G 1Estrogen Receptor/ERRInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    G-1
    Cat. No.:
    HY-107216
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (622 KB) Français - FR (622 KB) Deutsch - DE (622 KB) Norwegian - NO (622 KB) Español - ES (622 KB) Swedish - SV (622 KB) Italian - IT (622 KB) Korean - KR (622 KB) Portuguese - PT (622 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.