G-36 |
Catalog No.GC14902
One-Click Copy Product Info
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G-36 is a cell-permeable G protein-coupled estrogen receptor (GPER/GPR30) antagonist that inhibits estrogen-mediated calcium mobilization (IC50=112nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1392487-51-2
Sample solution is provided at 25 µL, 10mM.
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G-36 is a cell-permeable G protein-coupled estrogen receptor (GPER/GPR30) antagonist that inhibits estrogen-mediated calcium mobilization (IC50=112nM)[1-2]. G-36 can be used in research on cancer-related signaling pathways[3-4].
In vitro, pretreatment of human umbilical vein endothelial cells (HUVECs) with G-36 (1μM) completely blocked the ethinylestradiol (EE) and estetrol (E4) (1nM–100nM)-induced cell migration and inhibited the accumulation of phosphorylated focal adhesion kinase at tyrosine 397 (FAK Y397)[5]. Treatment of human cervical squamous cell carcinoma (CSCC) cell lines SiHa and C33A with G-36 (1–5μM) for 3 to 7 days had no significant effect on cell migration, colony formation, or tumor spheroid formation; however, treatment of SiHa cells with 2.5μM G-36 significantly increased the protein expression of plasminogen activator inhibitor-1 (PAI-1)[6].
In vivo, G-36 (0.5mg/kg) was co-administered with G-1 via intraperitoneal injection to high-fat diet (HFD)-fed C57BL/6 male mice (5 times per week for 5 weeks). G-36 blocked the protective effects of G-1 against HFD-induced obese asthma, reversing G-1's effects on airway hyperresponsiveness (AHR), pulmonary immune cell infiltration, tissue inflammation, fibrosis, mucus hypersecretion, increases in pro-inflammatory M1 macrophages, and decreases in anti-inflammatory M2 macrophages[7]. In ovariectomized C57Bl6 female mice, a single subcutaneous injection of G-36 (50μg/kg) blocked the G-1 (10μg/kg)-induced proliferation of uterine epithelial cells and significantly reduced the 17β-estradiol (E2; 10μg/kg)-induced proliferation[8].
References:
[1] Meyer MR, Barton M. GPER blockers as Nox downregulators: A new drug class to target chronic non-communicable diseases. J Steroid Biochem Mol Biol. 2018 Feb;176:82-87.
[2] Yu X, Stallone JN, Heaps CL, et al. The activation of G protein-coupled estrogen receptor induces relaxation via cAMP as well as potentiates contraction via EGFR transactivation in porcine coronary arteries. PLoS One. 2018 Jan 23;13(1):e0191418.
[3] Sharma G, Mauvais-Jarvis F, Prossnitz ER. Roles of G protein-coupled estrogen receptor GPER in metabolic regulation. J Steroid Biochem Mol Biol. 2018 Feb;176:31-37.
[4] Evans PD. Rapid signalling responses via the G protein-coupled estrogen receptor, GPER, in a hippocampal cell line. Steroids. 2019 Dec;152:108487.
[5] Dama A, Baggio C, Trevisi L, et al. Regulation of human endothelial cell migration by oral contraceptive estrogen receptor ligands. Eur J Pharmacol. 2023 Apr 15;945:175591.
[6] Rörig L, Ruckriegl S, Gallwas J, et al. G Protein-coupled Estrogen Receptor 1 (GPER1) Regulates Expression of SERPINE1/PAI-1 and Inhibits Tumorigenic Potential of Cervical Squamous Cell Carcinoma Cells In Vitro. Cancer Genomics Proteomics. 2025 Jan-Feb;22(1):13-23.
[7] Son SE, Im DS. Activation of G Protein-Coupled Estrogen Receptor 1 (GPER) Attenuates Obesity-Induced Asthma by Switching M1 Macrophages to M2 Macrophages. Int J Mol Sci. 2024 Sep 2;25(17):9532.
[8] Dennis MK, Field AS, Burai R, et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66.
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial cells |
Preparation Method | HUVECs were grown in M199 medium supplemented with 15% FBS, ECGS, heparin, glutamine, and gentamicin. For experiments, cells were switched to phenol-free M199 medium with 5% FBS, ECGS, and heparin. HUVECs were treated with G-36 (1μM). |
Reaction Conditions | 1μM; 6h. |
Applications | G-36 completely abolished the enhancement of HUVEC migration induced by ethinylestradiol (EE) and estetrol (E4) in both scratch and Boyden chamber assays. G-36 also blocked the accumulation of phosphorylated FAK at tyrosine 397 (FAK Y397) induced by EE and E4. |
| Animal experiment [2]: | |
Animal models | Ovariectomized C57Bl6 female mice |
Preparation Method | Mice were ovariectomized at 10 weeks of age. At 12 days post-ovariectomy, mice were subcutaneously injected with G-36 (50μg/kg). Mice were sacrificed 18 hours after injection, and uterine epithelial proliferation was quantified by Ki-67 immunofluorescence. |
Dosage form | 50μg/kg; s.c.; single injection. |
Applications | G-36 completely abolished the G-1-induced proliferation of uterine epithelial cells and significantly reduced the E2-induced proliferation. G-36 alone had no effect on proliferation. |
References: | |
| Cas No. | 1392487-51-2 | SDF | |
| Chemical Name | (3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-8-isopropyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | ||
| Canonical SMILES | CC(C1=CC([C@]2([H])C=CC[C@]2([H])[C@]3([H])C4=CC(OCO5)=C5C=C4Br)=C(N3)C=C1)C | ||
| Formula | C22H22BrNO2 | M.Wt | 412.33 |
| Solubility | 1/mL in ethanol, 20mg/mL in DMSO, 30mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4252 mL | 12.1262 mL | 24.2524 mL |
| 5 mM | 485 μL | 2.4252 mL | 4.8505 mL |
| 10 mM | 242.5 μL | 1.2126 mL | 2.4252 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)