G15 inhibits GPER-mediated proliferation stimulated by 17β-estradiol (E2) in A549 and H1793 cell lines. G15 also inhibits the response of GPER stimulated by E2 and G1 in A549 and H1793 cell lines. G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice.
Ecotoxicol Environ Saf. 2021 Jan 15;208:111429.
Environ Pollut. 2021 Feb 1;270:116051.
|Source||ECOTOX ENVIRON SAFE 2021 Jan. Figure 6. G15 (Abmole Bioscience Inc, Houston, TX, USA)|
|Cell Lines||KGN cells|
|Results||We found that G15 (a GPER inhibitor) pretreatment significantly inhibited BPA-induced apoptosis of KGN cells, while MPP (an ERα inhibitor) and PHTPP (an ERβ inhibitor) pretreatment had no significant inhibitory effect on apoptosis|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 20 mg/mL|
|Storage||-20°C, protect from light, dry, sealed|
Estrogen Signaling in ERα-Negative Breast Cancer: ERβ and GPER.
Girgert R, et al. Front Endocrinol (Lausanne). 2019 Jan 9;9:781. PMID: 30687231.
G-Protein-Coupled Estrogen Receptor Antagonist G15 Decreases Estrogen-Induced Development of Non-Small Cell Lung Cancer.
Liu C, et al. Oncol Res. 2019 Feb 21;27(3):283-292. PMID: 28877783.
|Related Estrogen Receptor Products|
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.