G15

Biological Activity

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.

Product Citations

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  Ecotoxicol Environ Saf. 2021 Jan 15;208:111429.

  Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca 2+-ASK1-JNK pathway in human granulosa cell line KGN
  G15 purchased from AbMole

• 

  Environ Pollut. 2021 Feb 1;270:116051.

  Bisphenol AF induces apoptosis via estrogen receptor beta (ERβ) and ROS-ASK1-JNK MAPK pathway in human granulosa cell line KGN
  G15 purchased from AbMole

Customer Product Validations & Biological Datas

	Source	ECOTOX ENVIRON SAFE 2021 Jan. Figure 6. G15 (Abmole Bioscience Inc, Houston, TX, USA)
	Method	cell culture
	Cell Lines	KGN cells
	Concentrations	5 μM
	Incubation Time	1h
	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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

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.