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.

G-1 Chemical Structure

G-1 Chemical Structure

CAS No. : 881639-98-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
1 mg USD 55 In-stock
5 mg USD 103 In-stock
10 mg USD 165 In-stock
50 mg USD 495 In-stock
100 mg USD 715 In-stock
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500 mg   Get quote  

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Customer Review

Based on 24 publication(s) in Google Scholar

G-1 Related Antibodies

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

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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]
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%

COA (254 KB) LCMS (96 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
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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

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