Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist - GPR antagonist - GPR antagonist G15 For research use only.

G15

Synonyms: GRB-G15

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.

G15 Chemical Structure

G15 Chemical Structure

CAS No. 1161002-05-6

Purity & Quality Control

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

G15 Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description 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.
Targets
GPER [1]
In vitro
In vitro

G15 inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines. G15 inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines.[1]
Cell Research Cell lines A549, H1793 cell lines
Concentrations 0.1 μM, 1 μM, 10 μM
Incubation Time 2 days
Method

To investigate the effects of G15 on tumor cell proliferation, the growth of A549 and H1793 cells is examined using the CCK-8 assay after administering 1, 10, and 100 nM selective agonist G1 and 1, 10, and 100 nM E2, and 10 nM E2 with 0.1, 1, and 10 μM Ful and 10 nM G1 with 0.1, 1, and 10 μM G15.
In Vivo
In vivo

G15 decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02518932 Unknown status
Insulin Resistance
Elahi Dariush PhD|ICON plc|Massachusetts General Hospital|National Institute on Aging (NIA)
 March 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 370.24 Formula

C19H16BrNO2
CAS No. 1161002-05-6 SDF --
Smiles C1C=CC2C1C(NC3=CC=CC=C23)C4=CC5=C(C=C4Br)OCO5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 74 mg/mL ( (199.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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