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G-1

SKU: orb1308286

Description

G-1 is a nonsteroidal, high-affinity, and selective agonist for GPR30 (GPER), with a Ki value of 11 nM. This compound is employed in both in vitro and in vivo research to study GPER-mediated signaling in fields such as oncology, cardiology, endocrinology, and neuroscience, as documented in scientific literature.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number881639-98-1
MW412.28
Purity99.89%
FormulaC21H18BrNO3
SMILES[H][C@@]12CC=C[C@]1([H])c1cc(ccc1N[C@@H]2c1cc2OCOc2cc1Br)C(C)=O
TargetGPCR,Estrogen Receptor/ERR
SolubilityDMSO:120 mg/mL (291.06 mM);H2O:< 0.1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.85 mM)

Bioactivity

Target IC50
GPR30:(ki)11 nM
In Vivo
After 14 days post-injury, the results display that the Basso mouse scale scores are obviously higher in the G-1 group compared with the other groups (P<0.05). G-1 administration produces a statistically significant induce in tumor volume from day 14 post-treatment. Grafted tumors harvested after a three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle-treated animals. The number of caspase-3-positive cells in the cross-sections is counted, and G-1 group has fewer positive cells compared with the other groups (P<0.05), and there is no difference between the two groups (P>0.05).
In Vitro
Treatment with G-1 (10 μM and 100 μM; 48 and 72 h) obviously reduces cell proliferation (P<0.001). At 72 h, the IC50 value for G-1 is calculated to be 20 μM. Cell cycle analysis of H295R cells after 24 h of G-1 treatment shows a cell cycle arrest in the G2 phase. Treatment of A549 cells with G-1(20 μM) reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001). The presence of G-1 increases Bax expression while reduces Bcl-2.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

ERR, G 1, Estrogen Receptor/ERR, EstrogenReceptor, Estrogen Receptor, GPR30, G1, G-1, inhibit, Inhibitor

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Key Properties

No computed properties available.

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G-1 (orb1308286)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,170.00
1 ml x 10 mM (in DMSO)
¥ 1,560.00
5 mg
¥ 1,560.00
10 mg
¥ 2,210.00
25 mg
¥ 3,380.00
50 mg
¥ 4,940.00
100 mg
¥ 6,890.00
200 mg
¥ 9,620.00
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