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G-1 目录号 GC12766

GPR30 agonist, potent and selective

规格 价格 库存 购买数量
1mg
¥315.00
现货
5mg
¥1,184.00
现货
10mg
¥1,890.00
现货
25mg
¥4,334.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

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.

Chemical Properties

Cas No. 881639-98-1 SDF
别名 N/A
化学名 rel-1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4S,5,9bS-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone
Canonical SMILES CC(C1=CC([C@@](C=CC2)([H])[C@@]2([H])[C@H](C3=CC(OCO4)=C4C=C3Br)N5)=C5C=C1)=O
分子式 C21H18BrNO3 分子量 412.28
溶解度 1mg/ml in ethanol; 20mg/ml in DMSO; 30mg/ml in DMF 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

G-1 is a potent and selective agonist of GPR30 with EC50 value of 2 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-1 is a potent and selective GPR30 agonist. In GPR30-expressing cells, G-1 competed binding of the fluorescent estrogen with Ki value of 11 nM, while no substantial binding at concentrations up to 1 μM in ERɑ- and ERβ-expressing cells. In GPR30-expressing COS7 cells, G-1 significantly increased intracellular calcium concentrations with EC50 value of 2 nM in a dose-dependent way. In SKBr3 breast cancer cells that expressed only GPR30, G-1 activated PI3K and resulted in the nuclear accumulation of PIP3 [1].

In female Sprague–Dawley rats with bilateral ovariectomy (OVX), ISO (85 mg/kg for 17 days) was given to make the heart failure models. G-1 (120 μg/kg for 14 days) treatment reduced cardiac fibrosis and concentration of brain natriuretic peptide and increased contraction of the heart. Also, G-1 increased the expression of β2-AR and normalized the expression of β1-AR [2].

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.