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G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $43 | In Stock | In Stock | |
| 5 mg | $77 | In Stock | In Stock | |
| 10 mg | $123 | In Stock | In Stock | |
| 25 mg | $213 | In Stock | In Stock | |
| 50 mg | $338 | In Stock | In Stock | |
| 100 mg | $488 | In Stock | In Stock | |
| 200 mg | $698 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $75 | In Stock | In Stock |
| Description | G-1 is a nonsteroidal, high-affinity, and selective GPR30 agonist (Ki: 11 nM). |
| Targets&IC50 | GPR30:(ki)11 nM |
| 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)[2]. The presence of G-1 increases Bax expression while reduces Bcl-2[3]. |
| 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[3]. 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)[1]. |
| Molecular Weight | 412.28 |
| Formula | C21H18BrNO3 |
| Cas No. | 881639-98-1 |
| Smiles | [H][C@@]12CC=C[C@]1([H])c1cc(ccc1N[C@@H]2c1cc2OCOc2cc1Br)C(C)=O |
| Relative Density. | 1.457 g/cm3 (Predicted) |
| Storage | store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 120 mg/mL (291.06 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.85 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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