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G-15

G-15

Catalog No.

B5469

GPER receptor antagonist

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Size	Price	Stock	Qty
10mg	$140.00	In stock

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Background
Product Citation
Chemical Properties
Protocol
Quality Control

Background

G-15 is a selective antagonist of GPR30 with Ki value of 20 nM [1].

G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].

G-15 is a selective GPR30 antagonist with Ki value of 20 nM, While displayed little binding to ERα or ERβ up to 10 μM. In SKBr3 breast cancer cells that expressed only GPR30, G-1 or estrogen significantly increased intracellular calcium concentrations, while G15 inhibited the response to G-1 or estrogen with IC50 value of 185 and 190 nM respectively in a dose-dependent way. In GPR30-transfected COS7 cells, G-15 inhibited both estrogen and G-1 activation of PI3K and accumulation of PIP3 [1]. In endometriotic cells, G-1 increased cell proliferation and Akt phosphorylation, while G-15 reversed this stimulation and inhibited cell proliferation and induced Akt dephosphorylation [2].

In intact rats and ovariectomized (OVX) rats treated with estradiol, G-15 impaired acquisition of delayed matching-to-position (DMP) T-maze task with a persistent turn. The result suggested that GPR30 played an crucial role in mediating the effects of estradiol on spatial learning [3].

References:
[1] Dennis MK, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist. Nat Chem Biol, 2009, 5 (6): 421-427.
[2] G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells. Fertil Steril, 2013, 100 (3): 770-776.
[3] Hammond R, Nelson D, Kline E, et al. Chronic treatment with a GPR30 antagonist impairs acquisition of a spatial learning task in young female rats. Horm Behav, 2012, 62 (4): 367-374.

Product Citation

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Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	370.24
Cas No.	1161002-05-6
Formula	C₁₉H₁₆BrNO₂
Solubility	insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO
Chemical Name	(3aR,4S,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
SDF	Download SDF
Canonical SMILES	BrC1=C([C@H]2NC3=CC=CC=C3[C@]4([H])[C@@]2([H])CC=C4)C=C5OCOC5=C1
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1,2]:
Cell lines	Immortalized epithelial endometriotic cell line (11z)
Preparation method	The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.
Reacting condition	10, 30, or 60 μM for 24, 48, or 72 hours
Applications	G-1 (30 μM) led to Akt phosphorylation at serine 473 within 2 hours. Pretreatment with G-15 (60 μM) prevented this phosphorylation by G-1. Treatment with 10 μM G-1 for 72 hours significantly stimulated the cells with an increase of the relative proliferation. A subsequent 72-hour treatment with 30 μM G-15 significantly reversed this stimulation. Treatment with G-15 alone led to a decrease of the relative proliferation. G-15 dose-dependently inhibited G-1-mediated calcium mobilization in SKBr3 cells with IC50 of ~185 nM. G15 inhibited the G-1-mediated activation of PI (3) K in GPR30-transfected COS7 cells.
Animal experiment [3]:
Animal models	Ovariectomized female rats
Dosage form	Subcutaneous injection, 5 μg/day, 10 μg/day
Application	G-15 dose-dependently impaired DMP acquisition. G-15 specifically reduced the rate of acquisition.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1] Imesch P, Samartzis E P, Dedes K J, et al. Histone deacetylase inhibitors down-regulate G-protein-coupled estrogen receptor and the GPER-antagonist G-15 inhibits proliferation in endometriotic cells [J]. Fertility and sterility, 2013, 100 (3): 770-776. [2] Dennis M K, Burai R, Ramesh C, et al. In vivo effects of a GPR30 antagonist [J]. Nature chemical biology, 2009, 5 (6): 421-427. [3] Hammond R, Nelson D, Kline E, et al. Chronic treatment with a GPR30 antagonist impairs acquisition of a spatial learning task in young female rats [J]. Hormones and behavior, 2012, 62 (4): 367-374.