Cat. No.: HY-107216

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G-1

30 Cited Publications

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Based on 30 publication(s) in Google Scholar

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

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

Purity: 99.76%
CAS No.: 881639-98-1
Formula: C₂₁H₁₈BrNO₃
Molecular Weight:412.28

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

G-1 Chemical Structure

CAS No.: 881639-98-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (30)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target

Ki: 11 nM (GPR30)^[1]

All Estrogen Receptor/ERR Isoforms :

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 K_i 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.

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.

Chemical Information

CAS No. 881639-98-1
Appearance Solid
Molecular Weight 412.28
Formula C₂₁H₁₈BrNO₃
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

Publications (30)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayBio/Physico-chemical AssayCell Imaging/StainingWB

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Journal Impact Factor

Cell Death Dis

Dehydroepiandrosterone exacerbates nigericin-induced abnormal autophagy and pyroptosis via GPER activation in LPS-primed macrophages. [Abstract]

2022 Apr 19;13(4):372. PMID: 35440074
Phytomedicine

Sweroside promotes osteoblastic differentiation and mineralization via interaction of membrane estrogen receptor-α and GPR30 mediated p38 signalling pathway on MC3T3-E1 cells. [Abstract]

2020 Mar:68:153146. PMID: 32028183
J Hazard Mater

Selenium restored mitophagic flux to alleviate cadmium-induced hepatotoxicity by inhibiting excessive GPER1-mediated mitophagy activation. [Abstract]

2024 Aug 15:475:134855. PMID: 38880044
Mol Psychiatry

Estrogen receptor beta in lateral habenula mediates antidepressant effects of estrogen in postpartum-hormone-withdrawal-induced depression. [Abstract]

2025 Sep 5. PMID: 40913111

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).
Cell Death Discov

Estrogens revert neutrophil hyperplasia by inhibiting Hif1α-cMyb pathway in zebrafish myelodysplastic syndromes models. [Abstract]

2022 Jul 16;8(1):323. PMID: 35842445
Mol Med

G protein-coupled estrogen receptor activates PI3K/AKT/mTOR signaling to suppress ferroptosis via SREBP1/SCD1-mediated lipogenesis. [Abstract]

2024 Feb 21;30(1):28. PMID: 38383297

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.
Clin Sci

Unravelling the effects of selective estrogen receptor modulators on colorectal cancer: a prognostic role for insulin-like growth factor binding protein-5. [Abstract]

2026 Jun 10;140(6):1011-1032. PMID: 42047268
CNS Neurosci Ther

Activation of GPER1 by G1 prevents PTSD-like behaviors in mice: Illustrating the mechanisms from BDNF/TrkB to mitochondria and synaptic connection. [Abstract]

2024 Jul;30(7):e14855. PMID: 38992889
Life Sci

Genistein accelerates glucose catabolism via activation the GPER-mediated cAMP/PKA-AMPK signaling pathway in broiler chickens. [Abstract]

2022 Aug 15:303:120676. PMID: 35640778
Eur J Pharmacol

Estradiol reduced 5-HT reuptake by downregulating the gene expression of Plasma Membrane Monoamine Transporter (PMAT, Slc29a4) through estrogen receptor β and the MAPK/ERK signaling pathway. [Abstract]

2022 Jun 5;924:174939. PMID: 35398393
Int Immunopharmacol

Estrogen deficiency promotes neurodegeneration in female hemi-parkinsonian mice: The role of regulatory T cells. [Abstract]

2025 Feb 20:148:114104. PMID: 39862633
J Clin Endocrinol Metab

Organoid Cultures Derived From Patients With Papillary Thyroid Cancer. [Abstract]

2021 Apr 23;106(5):1410-1426. PMID: 33524147
Mediators Inflamm

G Protein-Coupled Receptor 30 Attenuates Neuronal Pyroptosis Induced by Subarachnoid Hemorrhage. [Abstract]

2025 Jul 21:2025:3585885. PMID: 40726812
J Cell Physiol

17β-Estradiol mediates TGFBR3/Smad2/3 signaling to attenuate the fibrosis of TGF-β1-induced bovine endometrial epithelial cells via GPER. [Abstract]

2024 Jan;239(1):166-179. PMID: 37991438
J Cell Physiol

G-protein-coupled estrogen receptor protects retinal ganglion cells via inhibiting endoplasmic reticulum stress under hyperoxia. [Abstract]

2021 May;236(5):3780-3788. PMID: 33151568
J Biochem Mol Toxicol

Inhibiting endoplasmic reticulum stress by activation of G-protein-coupled estrogen receptor to protect retinal astrocytes under hyperoxia. [Abstract]

2021 Feb;35(2):e22641. PMID: 32996202
Appl Biochem Biotechnol

ERα, but not ERβ and GPER, Mediates Estradiol-Induced Secretion of TSH in Mouse Pituitary. [Abstract]

2022 Jun;194(6):2492-2502. PMID: 35138554
Biol Reprod

G protein-coupled estrogen receptor promotes acrosome reaction via regulation of Ca2+ signaling in mouse sperm. [Abstract]

2022 Oct 11;107(4):1026-1034. PMID: 35774023
J Steroid Biochem Mol Biol

GPER agonist G-1 activates YAP to induce apoptosis in breast cancer cells. [Abstract]

2025 Apr:248:106693. PMID: 39914681
Steroids

Exploration of interaction property between nonylphenol and G protein-coupled receptor 30 based on molecular simulation and biological experiments. [Abstract]

2022 Dec:188:109114. PMID: 36154832
J Nat Med

Integrated network pharmacology and pharmacological evaluation to elucidate the effect and mechanism of the novel combination PMS in treatment of osteoporosis. [Abstract]

2026 May;80(3):555-564. PMID: 41927855
Mol Reprod Dev

Estrogen influences the transzonal projection assembly of cumulus-oocyte complexes through G protein-coupled estrogen receptor during goat follicle development. [Abstract]

2024 Jun;91(6):e23763. PMID: 38895803
Int J Endocrinol

G Protein-Coupled Estrogen Receptor 1 (GPER1) Mediates Aldosterone-Induced Endothelial Inflammation in a Mineralocorticoid Receptor-Independent Manner. [Abstract]

2021 Jun 18:2021:5575927. PMID: 34239558
J Histotechnol

G protein-coupled receptor 30 activation protects hepatic ischemia-reperfusion injury of liver tissue through inhibiting NLRP3 in the rat model. [Abstract]

2021 Mar;44(1):27-36. PMID: 33210578
Johns Hopkins University

2025 Sep.
Evid Based Complement Alternat Med

Shikonin Mediates Apoptosis through G Protein-Coupled Estrogen Receptor of Ovarian Cancer Cells. [Abstract]

2022 Oct 5:2022:6517732. PMID: 36248433
J Cancer Ther

Breast Cancer MCF-7 Cell Spheroid Culture for Drug Discovery and Development. [Abstract]

2022 Mar;13(3):117-130. PMID: 36311820
J Oncol

GPR30 Activation Promotes the Progression of Gastric Cancer and Plays a Significant Role in the Anti-GC Effect of Huaier. [Abstract]

2022 Jan 19:2022:2410530. PMID: 35096058
Research Square Preprint

2021 Dec.
Aging (Albany NY)

G-protein coupled estrogen receptor activation protects the viability of hyperoxia-treated primary murine retinal microglia by reducing ER stress. [Abstract]

2020 Sep 13;12(17):17367-17379. PMID: 32920550

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4255 mL

12.1277 mL

24.2554 mL

5 mM

0.4851 mL

2.4255 mL

4.8511 mL

10 mM

0.2426 mL

1.2128 mL

2.4255 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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 N1^nu 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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (622 KB)
- 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cheng Q, et al. G-1 exerts neuroprotective effects through G protein-coupled estrogen receptor 1 following spinal cord injury in mice. Biosci Rep. 2016 Aug 31;36(4). pii: e00373. [Content Brief]

[2]. Kurt AH, et al. Oxidative/antioxidative enzyme-mediated antiproliferative and proapoptotic effects of the GPER1 agonist G-1 on lung cancer cells. Oncol Lett. 2015 Nov;10(5):3177-3182. [Content Brief]

[3]. Chimento A, et al. GPER agonist G-1 decreases adrenocortical carcinoma (ACC) cell growth in vitro and in vivo. Oncotarget. 2015 Aug 7;6(22):19190-203. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) G-1

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (30)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

G-1

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) G-1

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (30)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

G-1 Related Classifications

HY-107216 Related Classifications