G-1
Based on 29 publication(s) in Google Scholar
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.
- Purity: 99.76%
- CAS No.: 881639-98-1
- Formula: C21H18BrNO3
- Molecular Weight:412.28
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) G-1
More- J Hazard Mater. 2024 Jun 13:475:134855. [Abstract]
- Mol Psychiatry. 2025 Sep 5. [Abstract]
- Cell Death Dis. 2022 Apr 19;13(4):372. [Abstract]
- Phytomedicine. 2020 Mar;68:153146. [Abstract]
- Clin Sci. 2026 Jun 10;140(6):1011-1032. [Abstract]
- Cell Death Discov. 2022 Jul 16;8(1):323. [Abstract]
- Mol Med. 2024 Feb 21;30(1):28. [Abstract]
- Life Sci. 2022 Aug 15:303:120676. [Abstract]
- J Clin Endocrinol Metab. 2021 Apr 23;106(5):1410-1426. [Abstract]
- CNS Neurosci Ther. 2024 Jul;30(7):e14855. [Abstract]
- Int Immunopharmacol. 2025 Jan 24:148:114104. [Abstract]
- Eur J Pharmacol. 2022 Jun 5;924:174939. [Abstract]
- Mediators Inflamm. 2025 Jul 21:2025:3585885. [Abstract]
- J Cell Physiol. 2024 Jan;239(1):166-179. [Abstract]
- J Cell Physiol. 2021 May;236(5):3780-3788. [Abstract]
- Aging. 2020 Sep 13;12(17):17367-17379. [Abstract]
- Appl Biochem Biotechnol. 2022 Jun;194(6):2492-2502. [Abstract]
- Mol Reprod Dev. 2024 Jun;91(6):e23763. [Abstract]
- Biol Reprod. 2022 Oct 11;107(4):1026-1034. [Abstract]
- J Biochem Mol Toxicol. 2021 Feb;35(2):e22641. [Abstract]
- J Steroid Biochem Mol Biol. 2025 Feb 4:106693. [Abstract]
- Steroids. 2022 Dec:188:109114. [Abstract]
- Int J Endocrinol. 2021 Jun 18:2021:5575927. [Abstract]
- J Histotechnol. 2021 Mar;44(1):27-36. [Abstract]
- Johns Hopkins University. 2025 Sep.
- Evid Based Complement Alternat Med. 2022 Oct 5:2022:6517732. [Abstract]
- J Cancer Ther. 2022 Mar;13(3):117-130. [Abstract]
- J Oncol. 2022 Jan 19:2022:2410530. [Abstract]
- Research Square Preprint. 2021 Dec.
Customer Validation & Images
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
Biological Activity
Ki: 11 nM (GPR30)[1]
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Cell Line
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Type | Value | Description | References |
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| COS-7 | EC50 |
2 nM
Compound: 1, G-1
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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
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[PMID: 16520733] |
| MCF7 | IC50 |
1.6 nM
Compound: 1, G-1
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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
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[PMID: 16520733] |
| SK-BR-3 | IC50 |
0.7 nM
Compound: 1, G-1
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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
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[PMID: 16520733] |
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 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
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CAS No. 881639-98-1
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Appearance Solid
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Molecular Weight 412.28
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Formula C21H18BrNO3
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Color White to off-white
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SMILES
BrC1=C([C@H]2[C@]3([H])[C@](C=CC3)([H])C4=CC(C(C)=O)=CC=C4N2)C=C5C(OCO5)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (29)
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Journal Impact Factor
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Most Recent
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J Hazard Mater
Selenium restored mitophagic flux to alleviate cadmium-induced hepatotoxicity by inhibiting excessive GPER1-mediated mitophagy activation. [Abstract]2024 Jun 13:475:134855. 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).
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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 -
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 -
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.
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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 -
J Clin Endocrinol Metab
2021 Apr 23;106(5):1410-1426. PMID: 33524147 -
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 -
Int Immunopharmacol
Estrogen deficiency promotes neurodegeneration in female hemi-parkinsonian mice: The role of regulatory T cells. [Abstract]2025 Jan 24:148:114104. PMID: 39862633 -
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 -
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 -
Aging
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 -
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 -
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 -
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 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 -
J Steroid Biochem Mol Biol
2025 Feb 4:106693. 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 -
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 -
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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
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 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (12.13 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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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)
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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]
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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