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G-1

G-1

Catalog No.

B5455

GPR30 agonist, potent and selective

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Size	Price	Stock	Qty
10mg	$177.00	In stock

For scientific research use only and should not be used for diagnostic or medical purposes.

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Background
Product Citation
Chemical Properties
Protocol
Quality Control

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

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Chemical Properties

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	412.28
Cas No.	881639-98-1
Formula	C₂₁H₁₈BrNO₃
Solubility	≥41.2 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name	1-((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
SDF	Download SDF
Canonical SMILES	CC(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 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]:
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.