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Purity: =99.84%
| Targets |
G-15 targets the G protein-coupled estrogen receptor 1 (GPER/GPR30). GPER is a membrane receptor that mediates estrogen signaling. By binding to GPER with a Ki of 20 nM, G-15 blocks the activation of GPER by estrogen and other agonists. This inhibition prevents GPER-mediated signaling pathways, including those involved in cell proliferation and migration. Its selectivity for GPER over classical estrogen receptors makes it a valuable tool for studying GPER biology.
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| ln Vitro |
A549 and H1793 cell lines' GPER-mediated proliferation is inhibited by G15 (0.1–10 μM; 2 days) in response to 17β-estradiol (E2) [1]. G15 inhibits H1793 and A549 cell lines at 1 μM for 48 hours.
In vitro, G-15 is a high-affinity and selective GPER antagonist with a Ki of 20 nM. It competes with GPER for ligand binding sites, blocking the action of hormones on the receptor. This inhibits cell growth, proliferation, or migration. G-15 effectively blocks GPER-mediated signaling and proliferation induced by 17β-estradiol (E2) or the GPER agonist G1 in cancer cell lines such as A549 and H1793. It displays little binding affinity to ERα or ERβ at 10 μM. |
| ln Vivo |
In formate-induced adenocarcinoma inflammation, G15 (1.46 mg/kg; ih; twice weekly for 14 weeks) decreases the increased nodule number and tumor index in E2 or G1 group tumors [1].
In vivo, G-15 inhibits the anti-depressive effects of estrogen. As a GPER antagonist, it modulates estrogen signaling through this receptor. Its effects on GPER-mediated processes have been observed in preclinical models. The compound's in vivo activity supports its use as a tool for studying GPER function. Specific dosing regimens and detailed efficacy data are available in the scientific literature. |
| Enzyme Assay |
In vitro receptor binding assays for G-15 involve measuring its binding affinity to GPER using radioligand binding assays. Membranes from cells expressing GPER are incubated with radiolabeled estradiol and varying concentrations of G-15. The Ki value of 20 nM is determined from competition binding curves. Selectivity against ERα and ERβ is assessed using similar assays. Functional activity is assessed by measuring its ability to block GPER-mediated signaling events.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: A549, H1793 cell lines Tested Concentrations: 0.1, 1, 10μM (combined with 10nM E2) Incubation Duration: 2 days Experimental Results: Inhibition of GPER reaction. -E2 stimulus-mediated proliferation. Western Blot Analysis [1] Cell Types: A549, H1793 cell lines Tested Concentrations: 1 μM (combined with 10 nM E2 and 10 nM G1) Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of E2 and G1 stimulated GPER responses. In vitro cell-based assays for G-15 involve treating cells expressing GPER with the compound to assess its effects on GPER-mediated signaling and cell proliferation. Cells are stimulated with 17β-estradiol or the GPER agonist G1 in the presence or absence of G-15. GPER-mediated signaling is assessed by measuring downstream signaling events. Cell proliferation is measured using MTT or similar assays. These assays characterize the compound's GPER antagonist activity. |
| Animal Protocol |
Animal/Disease Models: 4weeks old female Kunming mice (urethane-induced adenocarcinoma) [1]
Doses: 1.46 mg/kg (combined with E2, 0.09 mg/kg and Fulvestrant (Ful), 2.4 mg/kg ) Method of Route of Administration: subcutaneous injection; twice a week for 14 weeks. Experimental Results: The number of tumor nodules in the E2+Ful+G15 group was diminished. In vivo animal experiments for G-15 have been conducted to study its effects on estrogen-mediated behaviors. The compound is typically administered via injection. Its ability to inhibit the anti-depressive effects of estrogen has been demonstrated. These studies support the compound's use as a tool for studying GPER function in vivo. |
| ADME/Pharmacokinetics |
G-15 has a molecular weight of 371.43 and a molecular formula of C22H21NO4. It is a high-affinity and selective GPER antagonist. The compound is soluble in DMSO at 64 mg/mL. It is typically dissolved in DMSO for in vitro studies and formulated for in vivo administration. Its pharmacokinetic properties have been characterized in preclinical studies. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for G-15 is not extensively reported. As a GPER antagonist, its safety profile is related to its effects on estrogen signaling through this receptor. The compound is generally well-tolerated in preclinical studies at therapeutic doses. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
G-15 is a high-affinity and selective GPER/GPR30 antagonist with a Ki of 20 nM. It displays little binding affinity to ERα or ERβ. G-15 inhibits GPER-mediated signaling and proliferation. It inhibits the anti-depressive effects of estrogen in vivo. The compound is a valuable tool for studying GPER biology.
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| Molecular Formula |
C19H16BRNO2
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|---|---|
| Molecular Weight |
370.246
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| Exact Mass |
369.036
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| CAS # |
1161002-05-6
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| PubChem CID |
7433743
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
462.7±45.0 °C at 760 mmHg
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| Flash Point |
233.7±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.649
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| LogP |
4.49
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
484
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1C=C[C@@H]2[C@H]1[C@@H](NC3=CC=CC=C23)C4=CC5=C(C=C4Br)OCO5
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| InChi Key |
YOLTZIVRJAPVPH-MJLGCCKJSA-N
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| InChi Code |
InChI=1S/C19H16BrNO2/c20-15-9-18-17(22-10-23-18)8-14(15)19-13-6-3-5-11(13)12-4-1-2-7-16(12)21-19/h1-5,7-9,11,13,19,21H,6,10H2/t11-,13-,19+/m0/s1
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| Chemical Name |
(3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
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| Synonyms |
G 15; G15; G-15
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~41.67 mg/mL (~112.55 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7009 mL | 13.5044 mL | 27.0088 mL | |
| 5 mM | 0.5402 mL | 2.7009 mL | 5.4018 mL | |
| 10 mM | 0.2701 mL | 1.3504 mL | 2.7009 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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