G15 Estrogen/progestogen Receptor antagonist

Cat.No.S6651

G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
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Quality Control

Batch: S665101 DMSO]74 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.35%
99.35

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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 ddH2O, 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.

Chemical Information, Storage & Stability

Molecular Weight 370.24 Formula

C19H16BrNO2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1161002-05-6 -- Storage of Stock Solutions

Synonyms GRB-G15 SMILES C1C=CC2C1C(NC3=CC=CC=C23)C4=CC5=C(C=C4Br)OCO5

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
GPER
In vitro

G15 inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines. This compound inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines.

In vivo

G15 decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-06)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07050017 COMPLETED
Appetite; Energy Intake; Post-exercise; Negative Energy Balance
Hacettepe University
2025-05-29
NCT05173259 COMPLETED
Chewing Problem; Mastication Disorder
University of Barcelona
2021-12-01
NCT03753022 UNKNOWN
Coronary Artery Disease; Coronary Artery Bypass Grafting; Acute Lung Injury
Federal University of São Paulo
2012-01
NCT04130893 TERMINATED
Vasoconstriction Disorder of Extremities
Hôpital Européen Marseille
2019-01-17
NCT02518932 UNKNOWN
Insulin Resistance
Elahi, Dariush, PhD
2015-03 PHASE1
NCT02518932 Unknown status
Insulin Resistance
Elahi Dariush PhD|ICON plc|Massachusetts General Hospital|National Institute on Aging (NIA)
2015-03 Phase 1

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