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G-1

Catalog No.
B5455
GPR30 agonist, potent and selective
Grouped product items
SizePriceStock Qty
10mg
$177.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

G-1 (CAS 881639-98-1) is a selective agonist for the G protein-coupled receptor GPR30. GPR30, an integral membrane receptor localized within the endoplasmic reticulum, binds estradiol and aldosterone and activates various intracellular signaling cascades. G-1 binds selectively to GPR30 with a Ki of approximately 11 nM, while exhibiting minimal affinity to estrogen receptors ERα and ERβ even at micromolar concentrations. Activation of GPR30 by G-1 elevates intracellular calcium concentrations (EC50 = 2 nM) and induces PI3K-dependent nuclear accumulation of PIP3. In animal models, G-1 treatment mitigates myocardial fibrosis, modulates β-adrenoceptor expression, and improves cardiac function, suggesting utility in cardiovascular and endocrine research.

Product Citation

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt412.28
Cas No.881639-98-1
FormulaC21H18BrNO3
Solubility≥41.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethan-1-one
SDFDownload SDF
Canonical SMILESCC(C1=CC=C(C([C@@]2([H])[C@]3([H])CC=C2)=C1)N[C@H]3C4=C(Br)C=C(OCO5)C5=C4)=O
Shipping ConditionSmall 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]:

Cell lines

SKBr3 breast cancer cells and MCF7 cells

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 nM

Applications

In both SKBr3 cells expressing only GPR30 and MCF7 cells expressing GPR30 and ERα/β, G-1 induced nuclear accumulation of PIP3. Besides, G-1 inhibited migration of SKBr3 and MCF7 cells with IC50 values of 0.7 nM and 1.6 nM, respectively. Therefore, G-1 could selectively bind to GPR30 in the same cell where ERs were present, activating endogenously expressed GPR30 and resulting in various physiologic responses, such as inhibition of cell migration.

Animal experiment [2]:

Animal models

Female Sprague–Dawley rats with bilateral ovariectomy and heart failure

Dosage form

120 μg/kg; for 14 days

Applications

In female Sprague-Dawley rats with bilateral ovariectomy and heart failure, G-1 treatment reduced concentration of brain natriuretic peptide, inhibited cardiac fibrosis and promoted heart contraction. G-1 attenuated heart failure through chronic activation of the GPR30 which was mediated by normalizing the expression of β1-AR and up-regulating the expression of β2-AR.

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]. Bologa CG, Revankar CM, Young SM, et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nat Chem Biol, 2006, 2(4): 207-212.

[2]. Kang S, Liu Y, Sun D, et al. Chronic activation of the G protein-coupled receptor 30 with agonist G-1 attenuates heart failure. PLoS One, 2012, 7(10): e48185.

Quality Control

Chemical structure

G-1

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